GKI-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GKI-1  纯度: 99.25%

GKI-1是Greatwall (GWL)激酶抑制剂,抑制hGWLFL和hGWL-KinDom的IC50 分别为4.9 和 2.5 µM。GKI-1 可高效抑制 ROCK1IC50为11 µM, 仅微弱抑制 PKA。

GKI-1

GKI-1 Chemical Structure

CAS No. : 2444764-03-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4950 In-stock
5 mg ¥4500 In-stock
10 mg ¥7500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GKI-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library

生物活性

GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA[1].

IC50 & Target

IC50: 4.9 µM (hGWLFL), 4.9 µM (hGWL-KinDom)[1]

体外研究
(In Vitro)

GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1].

Treatment of HeLa cells (25 and 50 µM, 0-8.5 hours) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

269.73

Formula

C15H12ClN3

CAS 号

2444764-03-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 200 mg/mL (741.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7074 mL 18.5371 mL 37.0741 mL
5 mM 0.7415 mL 3.7074 mL 7.4148 mL
10 mM 0.3707 mL 1.8537 mL 3.7074 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (18.54 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (18.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (18.54 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (18.54 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (8.05 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (8.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Ocasio CA, et al. A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct. Oncotarget. 2016 Nov 1;7(44):71182-71197.

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β-NETA

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

β-NETA  纯度: ≥98.0%

β-NETA 是一种有效的,非竞争性的胆碱乙酰转移酶 (ChAIC50=76 μM) 和胆碱酯酶 (ChE; IC50=40 µM) 抑制剂。β-NETA 微弱的抑制乙酰胆碱酯 (AChE; IC50=1 mM)。

β-NETA

β-NETA Chemical Structure

CAS No. : 31059-54-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥880 In-stock
10 mg ¥800 In-stock
50 mg ¥2400 In-stock
100 mg ¥4000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

β-NETA 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC50=76 μM) and cholinesterase (ChE; IC50=40 µM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC50=1 mM)[1][2].

IC50 & Target

IC50: 76 μM (ChA); 40 µM (ChE); 1 mM (AChE)[1]

体外研究
(In Vitro)

β-NETA exhibits no effects at muscarinic receptors, ganglionic nicotinic receptors, skeletal muscular nicotinic receptors, cholinesterases or carnitine acetyltransferase at concentrations which inhibits ChA. At concentrations higher than the IC50 value to inhibit ChA, β-NETA antagonizes the effect of acetylcholine (ED50=100 µM), histamine and KCl-induced contractions in the guinea pig longitudinal ileal muscle[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

369.24

Formula

C16H20INO

CAS 号

31059-54-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 31.25 mg/mL (84.63 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7083 mL 13.5413 mL 27.0827 mL
5 mM 0.5417 mL 2.7083 mL 5.4165 mL
10 mM 0.2708 mL 1.3541 mL 2.7083 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Sastry BV, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.

    [2]. B V Sastry, et al. 2-(alpha-Naphthoyl)ethyltrimethylammonium iodide and its beta-isomer: new selective, stable and fluorescent inhibitors of choline acetyltransferase. J Pharmacol Exp Ther. 1988 Apr;245(1):72-80.

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M-110

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

M-110  纯度: 98.78%

M-110 是一种高选择性的,ATP 竞争性的 PIM 激酶抑制剂,M-110 对 PIM-3 抑制作用最好,IC50=47 nM。M-110 抑制 PIM-1 和 PIM-2 的IC50 为 2.5 μM。M-110 抑制前列腺癌细胞的增殖,IC50 为 0.6-0.9 μM。

M-110

M-110 Chemical Structure

CAS No. : 1395048-49-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3575 In-stock
5 mg ¥3250 In-stock
10 mg ¥5500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

M-110 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM[1].

体外研究
(In Vitro)

M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM[1]. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM[1].
M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation[1].
M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50 values of 0.6 to 0.8 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: DU-145 cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM.

Western Blot Analysis[1]

Cell Line: DU-145 cells
Concentration: 10 μM
Incubation Time: 18 hours
Result: Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3. 

分子量

445.94

Formula

C22H28ClN5O3

CAS 号

1395048-49-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (74.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2425 mL 11.2123 mL 22.4245 mL
5 mM 0.4485 mL 2.2425 mL 4.4849 mL
10 mM 0.2242 mL 1.1212 mL 2.2425 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.61 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol Cancer Ther. 2010 Sep;9(9):2478-87.

    [2]. He Y, et al. Schisantherin A suppresses osteoclast formation and wear particle-induced osteolysis via modulating RANKL signaling pathways. Biochem Biophys Res Commun. 2014 Jul 4;449(3):344-50.

    [3]. Zhou E, et al. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Int Immunopharmacol. 2014 Sep;22(1):133-40.

    [4]. Sa F, et al. Discovery of novel anti-parkinsonian effect of schisantherin A in in vitro and in vivo. Neurosci Lett. 2015 Apr 23;593:7-12.

    [5]. Zhang LQ, et al. Schisantherin A protects against 6-OHDA-induced dopaminergic neuron damage in zebrafish and cytotoxicity in SH-SY5Y cells through the ROS/NO and AKT/GSK3β pathways. J Ethnopharmacol. 2015 Apr 29. pii: S0378-8741(15)00306-2.

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Ilginatinib hydrochloride(Synonyms: NS-018 hydrochloride)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ilginatinib hydrochloride (Synonyms: NS-018 hydrochloride) 纯度: ≥98.0%

Ilginatinib hydrochloride (NS-018 hydrochloride) 是一种高度有效的,可口服的 JAK2 抑制剂,IC50 值为 0.72 nM,对其选择性是对 JAK1 的 46 倍 (IC50, 33 nM),JAK3 的 54 倍 (IC50, 39 nM),以及 Tyk2 的 22 倍 (IC50, 22 nM)。

Ilginatinib hydrochloride(Synonyms: NS-018 hydrochloride)

Ilginatinib hydrochloride Chemical Structure

CAS No. : 1239358-85-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2951 In-stock
5 mg ¥3150 In-stock
10 mg ¥4750 In-stock
25 mg ¥9500 In-stock
50 mg ¥13500 In-stock
100 mg 询价

* Please select Quantity before adding items.

Ilginatinib hydrochloride 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-COVID-19 Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

IC50 & Target[1]

JAK2

0.72 nM (IC50)

Tyk2

22 nM (IC50)

JAK1

33 nM (IC50)

JAK3

39 nM (IC50)

体外研究
(In Vitro)

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib hydrochloride also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib hydrochloride shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2[1].
Ilginatinib hydrochloride (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib hydrochloride (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ilginatinib hydrochloride (NS-018 hydrochloride) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model[1].
Ilginatinib hydrochloride (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

425.89

Formula

C21H21ClFN7

CAS 号

1239358-85-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 35 mg/mL (82.18 mM)

H2O : 2 mg/mL (4.70 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3480 mL 11.7401 mL 23.4802 mL
5 mM 0.4696 mL 2.3480 mL 4.6960 mL
10 mM 0.2348 mL 1.1740 mL 2.3480 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.87 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29.

    [2]. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

Cell Assay
[2]

Bone marrow mononuclear cells (BMMNCs) from healthy volunteers and myelodysplastic syndrome (MDS) patients are incubated in MethoCult GF H4434 methylcellulose medium containing various hematopoietic cytokines at 1.0 × 105 cells/mL with or without Ilginatinib (NS-018) at 37°C in a humidified atmosphere of 5% CO2. Commercially available purified normal human CD34-positive (CD34+) BM cells are used as a control. Burst-forming unit-erythroid (BFU-E) and colonyforming unit-granulocyte/macrophage (CFU-GM) colonies are counted under an inverted microscope on day 14 of culture[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Female BALB/c nude mice are placed in blanket cages in an environment maintained at 21-25°C and 45-65% relative humidity, with artificial illumination for 12 h and a ventilation frequency of at least 15 times/h. They are allowed free access to food pellets and tap water. Ba/F3-JAK2V617F cells (106 per mouse) are inoculated intravenously into 7-week-old mice. Administration of vehicle (0.5% methylcellulose) or Ilginatinib (NS-018) twice daily by oral gavage begins the day after cell inoculation. Survival is monitored daily, and moribund mice are humanely killed and their time of death is recorded for purposes of survival analysis. In a parallel study, all mice are humanely killed after 8 days of administration, and their spleens are removed and weighed[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29.

    [2]. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

ERK5-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ERK5-IN-1  纯度: 99.92%

ERK5-IN-1 是一种有效的 ERK5 抑制剂,IC50 为 87±7 nM。ERK5-IN-1 也抑制 LRRK2 [G2019S],IC50 为 26 nM。

ERK5-IN-1

ERK5-IN-1 Chemical Structure

CAS No. : 1234479-76-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

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  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.

IC50 & Target[1]

ERK5

87 nM (IC50)

LRRK2[G2019S]

26 nM (IC50)

体外研究
(In Vitro)

ERK5-IN-1 (Compound 5) exhibits a cellular EC50 for inhibiting epidermal growth factor (EGF) induced ERK5 autophosphorylation of 0.19±0.04 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

459.54

Formula

C25H29N7O2

CAS 号

1234479-76-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (217.61 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1761 mL 10.8804 mL 21.7609 mL
5 mM 0.4352 mL 2.1761 mL 4.3522 mL
10 mM 0.2176 mL 1.0880 mL 2.1761 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.98 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.98 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.98 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767.

Kinase Assay
[1]

Kinase activity is determined in an assay volume of 40 μL in kinase buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction started by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays are carried out for 20 min at 30°C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767.

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Harmane(Synonyms: 哈尔满碱)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Harmane (Synonyms: 哈尔满碱) 纯度: 99.73%

Harmane,一种 β-咔啉生物碱 (BCA),是有效的神经毒素,可引起严重的动作震颤和精神病学表现。Harmane 对 I1 咪唑啉受体 (I1-Imidazoline receptor, IC50=30 nM) 的选择性是对 α2-肾上腺素受体 (IC50=18 μM) 的 1000 倍。Harmane 还是有效和选择性的单胺氧化酶抑制剂 (对 MAO A/BIC50 值分别为 0.5 μM 和 5 μM)。Harmane 具有致突变作用。

Harmane(Synonyms: 哈尔满碱)

Harmane Chemical Structure

CAS No. : 486-84-0

规格 价格 是否有货 数量
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500 mg   询价  

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  • Neurodegenerative Disease-related Compound Library
  • Mitochondria-Targeted Compound Library

生物活性

Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect[1][2][3][4].

IC50 & Target[2][3]

hMAO-A

0.5 μM (IC50)

MAO-B

5 μM (IC50)

α2-adrenergic receptor

18 μM (IC50)

I1-Imidazoline receptor

30 nM (IC50)

分子量

182.22

Formula

C12H10N2

CAS 号

486-84-0

中文名称

哈尔满碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (685.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.4879 mL 27.4394 mL 54.8787 mL
5 mM 1.0976 mL 5.4879 mL 10.9757 mL
10 mM 0.5488 mL 2.7439 mL 5.4879 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (11.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.41 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (11.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.41 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (11.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Louis ED, et, al. Blood harmane concentrations and dietary protein consumption in essential tremor. Neurology. 2005 Aug 9;65(3):391-6.

    [2]. Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9.

    [3]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications

    [4]. Umezawa K, et, al. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

MK-4101

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MK-4101  纯度: 98.31%

MK-4101 是一种 SMO 拮抗剂 (对 293 细胞的 IC50 为 1.1 µM),也是一种有效的 hedgehog 途径抑制剂 (对小鼠细胞的 IC50 为 1.5 µM;对 KYSE180 食管癌细胞的 IC50 为 1 µM)。MK-4101 具有强大的抗肿瘤活性,能抑制肿瘤细胞增殖并诱导细胞凋亡。

MK-4101

MK-4101 Chemical Structure

CAS No. : 935273-79-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1118 In-stock
2 mg ¥680 In-stock
5 mg ¥1030 In-stock
10 mg ¥1700 In-stock
25 mg ¥3200 In-stock
50 mg ¥5100 In-stock
100 mg ¥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis[1].

IC50 & Target

IC50: 1.1 µM (293 cells ); 1.5 µM (mouse cells); 1 µM (KYSE180 oesophageal cancer cells)[1]

体外研究
(In Vitro)

MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC50 of 1.5 µM, and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1-/+ mice in vitro with an IC50 of 0.3 µM[1].
MK-4101 (10 µM; 60 hours, 72 hours; medulloblastoma or BCC cells) treatment shows cell cycle arrest with a nearly complete disappearance of the S phase subpopulation, a prominent increase of the G1 population and, to a minor extent, of the G2 population[1].
MK-4101 (10 µM; medulloblastoma or BCC cells) treatment significantly reduces cyclin D1 protein and accumulation of cyclin B1 protein[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Medulloblastoma or BCC cells
Concentration: 10 µM
Incubation Time: 60 hours, 72 hours
Result: Showed cell cycle arrest.

Western Blot Analysis[1]

Cell Line: Medulloblastoma or BCC cells
Concentration: 10 µM
Incubation Time:
Result: Significant reduction of cyclin D1 protein and accumulation of cyclin B1 protein.

体内研究
(In Vivo)

MK-4101 (40-80 mg/kg; oral administration; for 3.5 weeks; CD1 nude female mice) treatment shows tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg). MK-4101 treatment shows a dose-dependent down-regulation of Gli1 mRNA. The maximum effect for tumor inhibition and hedgehog pathway downregulation is achieved at 80 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-weeks old CD1 nude female mice with medulloblastoma/BCC cells[1]
Dosage: 40 or 80 mg/kg once a day, 80 mg/kg twice a day
Administration: Oral administration; for 3.5 weeks
Result: Showed tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg).

分子量

493.47

Formula

C24H24F5N5O

CAS 号

935273-79-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (101.32 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0265 mL 10.1323 mL 20.2647 mL
5 mM 0.4053 mL 2.0265 mL 4.0529 mL
10 mM 0.2026 mL 1.0132 mL 2.0265 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.07 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.07 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Filocamo G et al. MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1177-89.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Vps34-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vps34-IN-2  纯度: 99.74%

Vps34-IN-2 是一种新型的,有效且有选择性的 Vps34 抑制剂,在 Vps34 酶促测定和 GFP-FYVE 细胞测定中的 IC50 值分别为 2 和 82 nM。Vps34-IN-2 对 SARS-CoV-2 (IC50 为 3.1 μM),HCoV-229E (IC50 为 0.7 μM) 和 HCoV-OC43 具有抗病毒活性。

Vps34-IN-2

Vps34-IN-2 Chemical Structure

CAS No. : 1523404-29-6

规格 价格 是否有货 数量
1 mg ¥1900 In-stock
5 mg ¥5900 In-stock
10 mg ¥8900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Vps34-IN-2 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library

生物活性

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively[1]. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43[2].

IC50 & Target[1][2]

Vps34

2 nM (IC50)

SARS-CoV-2

3.1 μM (IC50)

HCoV-229E

0.7 μM (IC50)

体外研究
(In Vitro)

Vps34-IN-2 (Compound 31) displays IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 exhibits selectivity against mTOR (IC50>10 μM) and class I PI3Ks (IC50 values of 2.7, 4.5, 2.5, and >10 μM on PI3K α, β, δ, γ isoforms, respectively)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

After administration by the intravenous (iv) route, Vps34-IN-2 (Compound 31) concentrations are quantifiable up to 6, 8, and 24 h (last sampling time) depending on animals. After oral administration (po), Vps34-IN-2 is rapidly absorbed with maximal plasma concentrations observed at 0.5 h and a bioavailability of 85%. Slight rebounds of concentrations are observed at 4 and 8 h after oral dosing with no obvious explanation. After iv injection of Vps34-IN-2 at 3 mg/kg, plasma clearance is found moderate (i.e., 2.3 L/h/kg), corresponding to 44% of hepatic blood flow in this species, volume of distribution at steady state is moderate, and terminal elimination half-life is short[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

402.41

Formula

C18H25F3N4O3

CAS 号

1523404-29-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

Ethanol : 50 mg/mL (124.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4850 mL 12.4251 mL 24.8503 mL
5 mM 0.4970 mL 2.4850 mL 4.9701 mL
10 mM 0.2485 mL 1.2425 mL 2.4850 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Pasquier B, et al. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors. J Med Chem. 2015 Jan 8;58(1):376-400.

    [2]. Jim Baggen, et al. Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2. Nat Genet. 2021 Mar 8.

Cell Assay
[1]

Cells are cultured in RPMI-1640 medium with 10% fetal bovine serum. Cells are lysed by sonication in a detergent containing lysis buffer and cleared by centrifugation, and the resulting supernatant is collected for compound treatment. Final protein concentration of lysates is 4 mg/mL. An amount of 5 μL of Vps34-IN-2 (Compound 31) is added from 100× stock solutions in DMSO to 445 μL of lysate in duplicate. An amount of 5 μL of DMSO is added to 445 μL of lysate in quadruplicate for controls. After 15 min incubation, 5 μL of a 100× aqueous solution of the ATP probe I is added to each sample (final concentration of ATP probe I is 0.5 μM). After 5 min, 50 μL of a 10× aqueous solution of the ATP probe II is added to each sample (final concentration of ATP probe II is 20 μM). All samples are then incubated for an additional 10 min[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

For PK/PD studies, 3×106 H1299-GFP-FYVE tumor cells with 50% Matrigel are subcutaneously injected on the dorsal side of SCID mice, one tumor per mouse. When xenografted tumors reach a range of ~200 to 400 mm3, mice are treated with vehicle (98% PEG200/2% PS80) or a single dose of Vps34-IN-2 (compound 31) at 100 and 50 mg/kg via oral gavage. Three mice treated with vehicle alone and three mice treated with Vps34-IN-2 are sacrificed at each time point; tumor tissues are harvested for immunohistochemistry (IHC) analysis and plasma samples are collected to determine the concentration of Vps34-IN-2[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Pasquier B, et al. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors. J Med Chem. 2015 Jan 8;58(1):376-400.

    [2]. Jim Baggen, et al. Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2. Nat Genet. 2021 Mar 8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

JND3229

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

JND3229  纯度: 99.38%

JND3229 是一种高效的 EGFRC797S 的第四代可逆抑制剂, IC50 值为 5.8 nM ,同时对于EGFR L858R/T790M 和 EGFRWT 的 IC50 值分别为 30.5 和 6.8 nM。

JND3229

JND3229 Chemical Structure

CAS No. : 2260886-64-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5360 In-stock
5 mg ¥3950 In-stock
10 mg ¥6050 In-stock
50 mg ¥18500 In-stock
100 mg ¥28000 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JND3229 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

JND3229 is a highly potent and fourth-generation EGFRC797S reversible inhibitor with IC50 value of 5.8 nM, and also potently suppressed EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 and 6.8 nM.

分子量

617.18

Formula

C33H41ClN8O2

CAS 号

2260886-64-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (20.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6203 mL 8.1014 mL 16.2027 mL
5 mM 0.3241 mL 1.6203 mL 3.2405 mL
10 mM 0.1620 mL 0.8101 mL 1.6203 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.03 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Lu X, et al. Discovery of JND3229 as a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy. ACS Med Chem Lett. 2018 Oct 8;9(11):1123-1127.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

AZ12672857

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AZ12672857  纯度: 98.44%

AZ12672857 是具有口服活性的 EphB4 (IC50=1.3 nM) 和 Src 激酶的抑制剂。AZ12672857 抑制 c-Src 转染 3T3 细胞的增殖 (IC50=2 nM) 和抑制转染 CHO-K1 细胞中的 EphB4 自磷酸化 (IC50=9 nM)。

AZ12672857

AZ12672857 Chemical Structure

CAS No. : 945396-55-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4280 In-stock
5 mg ¥4000 In-stock
10 mg ¥6800 In-stock
25 mg ¥13500 In-stock
50 mg ¥22000 In-stock
100 mg ¥34000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AZ12672857 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1].

IC50 & Target[1]

EP4

1.3 nM (IC50)

Src

 

体外研究
(In Vitro)

AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

486.57

Formula

C26H30N8O2

CAS 号

945396-55-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (51.38 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0552 mL 10.2760 mL 20.5520 mL
5 mM 0.4110 mL 2.0552 mL 4.1104 mL
10 mM 0.2055 mL 1.0276 mL 2.0552 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Bardelle C, et al. Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors. Bioorg Med Chem Lett. 2010;20(21):6242-6245.

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IN-1130

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

IN-1130  纯度: 99.79%

N-1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂,对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。IN-1130 抑制酪蛋白的 ALK5 磷酸化 (IC50=36 nM),抑制 p38α 丝裂原活化的蛋白激酶 (IC50=4.3 μM)。IN-1130 可抑制阻塞性肾病中的肾纤维化,阻止乳腺癌的肺转移。

IN-1130

IN-1130 Chemical Structure

CAS No. : 868612-83-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
25 mg ¥3500 In-stock
50 mg ¥5500 In-stock
100 mg ¥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library
  • Anti-Colorectal Cancer Compound Library

生物活性

IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis[1][2].

IC50 & Target[1]

ALK5

 

体外研究
(In Vitro)

IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells[2].
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells[2].
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: HepG2 and 4T1 cells
Concentration: 0.5, 1 μM
Incubation Time: For 2 hours
Result: Inhibited TGF-β-stimulated Smad2 phosphorylation.

RT-PCR[2]

Cell Line: MCF10A cells
Concentration: 1 μM
Incubation Time: For 72 hours
Result: Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.

体内研究
(In Vivo)

IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats[1].
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys[1].
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old male Sprague–Dawley rats weighing 180-200 g[1]
Dosage: 10 and 20 mg/kg
Administration: IP; daily; for 7 and 14 days
Result: Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

分子量

420.47

Formula

C25H20N6O

CAS 号

868612-83-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (237.83 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3783 mL 11.8915 mL 23.7829 mL
5 mM 0.4757 mL 2.3783 mL 4.7566 mL
10 mM 0.2378 mL 1.1891 mL 2.3783 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.43 mg/mL (3.40 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (3.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43.

    [2]. Park CY, et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80.

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ML339

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ML339  纯度: 99.88%

ML339 是一种选择性的 CXCR6 拮抗剂,IC50 为 140 nM。ML339 对 CXCR5,CXCR4,CCR6 和 Apelin 受体 (APJ) 的 IC50 >79 μM。ML339 具有推动前列腺癌研究领域发展的潜力。

ML339

ML339 Chemical Structure

CAS No. : 2579689-83-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ¥5000 In-stock
10 mg ¥8500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

ML339 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Targeted Diversity Library

生物活性

ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research[1].

IC50 & Target[1]

CXCR6

140 nM (IC50)

分子量

502.00

Formula

C26H32ClN3O5

CAS 号

2579689-83-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (249.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9920 mL 9.9602 mL 19.9203 mL
5 mM 0.3984 mL 1.9920 mL 3.9841 mL
10 mM 0.1992 mL 0.9960 mL 1.9920 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.14 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Paul M. Hershberger, et al. Probing the CXCR6/CXCL16 Axis: Targeting Prevention of Prostate Cancer Metastasis.

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NU6140

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NU6140  纯度: 99.51%

NU6140 是一种选择性的 CDK2-cyclin A 抑制剂 (IC50,0.41 μM),对其选择性是对其他 CDK 的 10-36 倍。NU6140 有效抑制 Aurora AAurora B 的活性,IC50 值分别为 67 和 35 nM。增强诱导凋亡的作用,抗肿瘤作用。

NU6140

NU6140 Chemical Structure

CAS No. : 444723-13-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1760 In-stock
5 mg ¥1600 In-stock
10 mg ¥2560 In-stock
25 mg ¥5100 In-stock
50 mg ¥8150 In-stock
100 mg ¥13050 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NU6140 相关产品

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  • Bioactive Compound Library Plus
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  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively[2]. Enhances the apoptotic effect, with anti-cancer activity[1][2].

IC50 & Target[1][2]

cdk2-cyclin A

0.41 μM (IC50)

CDK1-Cyclin B

6.6 μM (IC50)

CDK4-Cyclin D

5.5 μM (IC50)

cdk5-p25

15 μM (IC50)

cdk7-cyclin H

3.9 μM (IC50)

Aurora A

67 nM (IC50)

Aurora B

35 nM (IC50)

体外研究
(In Vitro)

NU6140 is less active on CDK1-cyclin B, CDK4-cyclin D, CDK5-p25 and CDK7-cyclin H, with IC50s of 6.6, 5.5, 15 and 3.9 μM, respectively[1].
NU6140 increases catalytic activity of capase-9 and capase-3, causes increase in the sub-G1 apoptotic cell population[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

422.52

Formula

C23H30N6O2

CAS 号

444723-13-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (591.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3668 mL 11.8338 mL 23.6675 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Pennati M, et al. Potentiation of apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37.

    [2]. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? Med Chem. 2018 Oct 25;61(20):9105-9120.

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Sophoflavescenol(Synonyms: 槐苦参醇)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Sophoflavescenol (Synonyms: 槐苦参醇) 纯度: 98.15%

Sophoflavescenol 是一种异戊烯基黄酮类化合物,能够抑制 PDE5 的活性,IC50 值为 0.013 μM;同时抑制 RLAR,HRAR,BACE1,AChE 和 BChE,IC50 值分别为 0.30 µM,0.17 µM,10.98 µM,8.37 µM 和 8.21 µM。

Sophoflavescenol(Synonyms: 槐苦参醇)

Sophoflavescenol Chemical Structure

CAS No. : 216450-65-6

规格 价格 是否有货 数量
1 mg ¥2200 In-stock
5 mg ¥6600 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Sophoflavescenol 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.

IC50 & Target

IC50: 0.013 μM (PDE5), 0.30 µM (RLAR), 0.17 µM (HRAR), 17.89 µg/mL (AGE), 10.98 µM (BACE1), 8.37 µM (AChE), 8.21 µM (BChE)

体外研究
(In Vitro)

Sophoflavescenol shows cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells. Sophoflavescenol exerts notable anti-inflammatory activity by inhibiting nitric oxide generation and tert-butylhydroperoxide-induced ROS generation rather than inhibiting nuclear factor kappa B activation in RAW 264.7 cells[1]. Sophoflavescenol exhibits remarkable inhibition of RLAR activity with an IC50 value of 0.30 µM, compared with 0.07 µM for epalrestat, a well known ARI. Sophoflavescenol also shows potent inhibitory activity with an IC50 value of 0.17 µM, comparable to epalrestat (0.15 µM) in the HRAR assay. In the AGE assay, sophoflavescenol (IC50 17.89 µg/mL) is a more potent inhibitor of AGE formation than aminoguanidine (IC50 81.05 µg/mL). Sophoflavescenol exerts both potent AChE and BChE inhibitory effects with respective IC50 values of 8.37 and 8.21 µM. Sophoflavescenol also exhibits good BACE1 inhibition in a dose-dependent manner with an IC50 value of 10.98 µM[2]. Sophoflavescenol is a mixed inhibitor (Ki=0.005 μM) against cGMP PDE5. Sophoflavescenol shows greatest selectivity toward PDE5, 31.5- and 196.2-fold over PDE3 and PDE4, respectively[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Sophoflavescenol exerts potent in vivo antitumor activity by tumor growth inhibition in the LLC tumor model as well as apoptotic activity by caspase-3 activation in HL-60 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

368.38

Formula

C21H20O6

CAS 号

216450-65-6

中文名称

槐黄醇;槐苦参醇

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL (67.86 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL
10 mM 0.2715 mL 1.3573 mL 2.7146 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.79 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.79 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Jung HA, et al. Anti-tumorigenic activity of sophoflavescenol against Lewis lung carcinoma in vitro and in vivo. Arch Pharm Res. 2011 Dec;34(12):2087-99

    [2]. Jung HA, et al. Antidiabetic complications and anti-Alzheimer activities of sophoflavescenol, a prenylated flavonol from Sophora flavescens, and its structure-activity relationship. Phytother Res. 2011 May;25(5):709-15.

    [3]. Shin HJ, et al. A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.

Kinase Assay
[2]

Briefly, a mixture of 10 µL of assay buffer (50 mm sodium acetate, pH 4.5), 10 µL of BACE1 (1.0 U/mL), 10 µL of the substrate (750 nm Rh-EVNLDAEFK-Quencher in 50 mm, ammonium bicarbonate) and 10 µL of the tested samples [final concentration (f.c.) 100 µM for compounds] dissolved in 10% DMSO is incubated for 60 min at 25°C in the dark. The proteolysis of two fluorophores (Rh-EVNLDAEFK-Quencher) by BACE1 is monitored by formation of the fluorescent donor (Rh-EVNL) that increased in fluorescence wavelengths at 530-545 nm (excitation) and 570-590 nm (emission), respectively. Fluorescence is measured with a microplate spectrofluorometer. The mixture is irradiated at 545 nm and the emission intensity recorded at 585 nm. The percent inhibition (%) is obtained by the following equation: % Inhibition=[1 − (S60 − S0)/(C60 − C0)] × 100, where C60 is the fluorescence of the control (enzyme, buffer, substrate) after 60 min of incubation, C0 the initial fluorescence of the control, S60 the fluorescence of the tested samples (enzyme, sample solution, substrate) after 60 min of incubation, and S0 the initial fluorescence of the tested samples. To allow for the quenching effect of the samples, the sample solution is added to reaction mixture C, and any reduction in fluorescence by the sample is then investigated. The BACE1 inhibitory activity of each sample is expressed in terms of the IC50 value (µM required to inhibit proteolysis of the BACE1 substrate, by 50%), as calculated from the log-dose inhibition curve.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Jung HA, et al. Anti-tumorigenic activity of sophoflavescenol against Lewis lung carcinoma in vitro and in vivo. Arch Pharm Res. 2011 Dec;34(12):2087-99

    [2]. Jung HA, et al. Antidiabetic complications and anti-Alzheimer activities of sophoflavescenol, a prenylated flavonol from Sophora flavescens, and its structure-activity relationship. Phytother Res. 2011 May;25(5):709-15.

    [3]. Shin HJ, et al. A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

LPA2 antagonist 2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

LPA2 antagonist 2  纯度: 95.03%

LPA2 antagonist 2 是一种选择性 LPA2 拮抗剂,IC50 为 28.3 nM,Ki 为 21.1 nM,比 LPA3 (IC50 为 13.85 μM) 选择性高 480 倍以上。

LPA2 antagonist 2

LPA2 antagonist 2 Chemical Structure

CAS No. : 36840-10-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2930 In-stock
1 mg ¥1200 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

LPA2 antagonist 2 相关产品

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生物活性

LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM)[1].

IC50 & Target

IC50: 28.3 nM (LPA2); 13.85 μM (LPA3)[1]

体外研究
(In Vitro)

Lysophosphatidic acid (LPA) is a phospholipid mediator that elicits a host of biological effects including cell proliferation, survival, motility and differentiation. LPA has been shown to regulate cancer cell invasion, metastasis, and resistance to both chemotherapeutics and radiation. LPA2 antagonist 2 (H2L 5226501) inhibits LPA1 with an Imax of 59.0% at 30 µM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

380.35

Formula

C20H16N2O6

CAS 号

36840-10-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (219.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6292 mL 13.1458 mL 26.2916 mL
5 mM 0.5258 mL 2.6292 mL 5.2583 mL
10 mM 0.2629 mL 1.3146 mL 2.6292 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Fells JI, et al. Identification of non-lipid LPA3 antagonists by virtual screening. Bioorg Med Chem. 2008 Jun 1;16(11):6207-17.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

X-376

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

X-376  纯度: 98.36%

X-376 是一种有效的高特异性 ALK 酪氨酸激酶抑制剂 (TKI) (IC50=0.61 nM)。X-376 是 MET 的较低效抑制剂 (IC50=0.69 nM)。X-376 具有有效的抗肿瘤活性。

X-376

X-376 Chemical Structure

CAS No. : 1365267-27-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥2649 In-stock
2 mg ¥1100 In-stock
5 mg ¥2200 In-stock
10 mg ¥3000 In-stock
25 mg ¥6600 In-stock
50 mg ¥11000 In-stock
100 mg 询价

* Please select Quantity before adding items.

X-376 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
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  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity[1].

IC50 & Target[1]

ALK

0.61 nM (IC50)

MET

0.69 nM (IC50)

体外研究
(In Vitro)

The ability of X-376 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-376 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 77 nM). X-376 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 57 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 32 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 142 nM, 150 nM, 15.137 μM and 3.062 μM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The effects of X-376 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-376 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-376 at 50 mg/kg bid. X-376 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-376 appears well-tolerated in vivo. Mouse weight is unaffected by X-376 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-376, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-376 at 25, 50, 100 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 50 mg/kg for X-376. At NST levels, X-376 achieves an AUC of 41 μM×hr and a Cmax of 5.04 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

547.41

Formula

C25H25Cl2FN6O3

CAS 号

1365267-27-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (182.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8268 mL 9.1339 mL 18.2678 mL
5 mM 0.3654 mL 1.8268 mL 3.6536 mL
10 mM 0.1827 mL 0.9134 mL 1.8268 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.57 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.57 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.57 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

Cell Assay
[1]

For viability experiments, cells are seeded in 96-well plates at 25%-33% confluency and exposed to drugs. The human lung adenocarcinoma cell lines H3122 and H2228 are treated with X-376 (10, 30, 100, 300 and 1000 nM). SUDHL-1 lymphoma cells are treated with X-376 (5, 10, 30, 100 and 300 nM). SY5Y neuroblastoma cells are treated with X-376 (30, 100, 300 and 1000 nM). At 72 hours post X-376 addition, Cell Titer Blue Reagent is added and fluorescence is measured on a Spectramax spectrophotometer. All experimental points are set up in hextuplicate replicates and are performed at least two independent times. IC50s are calculated using GraphPad Prism version 5 for Windows. The curves are fit using a nonlinear regression model with a log (inhibitor) vs. response formula[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Nude mice (nu/nu) are injected with H3122 cells. Once tumors reach an average volume of 450 mm3, a total of 27 athymic mice harboring H3122 tumors are randomized and dosed via oral gavage with 50 mg/kg X-376 or the control vehicle. Two, five, and fifteen hours after the single treatment (3 tumors/timepoint/group), mice are sacrificed and serum is collected for assessment of drug concentration using an LC-MS based bioanalytical method.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Ilginatinib maleate(Synonyms: NS-018 maleate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ilginatinib maleate (Synonyms: NS-018 maleate) 纯度: 97.04%

Ilginatinib maleate (NS-018 maleate) 是一种高度有效的,可口服的 JAK2 抑制剂,IC50 值为 0.72 nM,对其选择性是对 JAK1 的 46 倍 (IC50, 33 nM),JAK3 的 54 倍 (IC50, 39 nM),以及 Tyk2 的 22 倍 (IC50, 22 nM)。

Ilginatinib maleate(Synonyms: NS-018 maleate)

Ilginatinib maleate Chemical Structure

CAS No. : 1354799-87-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3503 In-stock
5 mg ¥3150 In-stock
10 mg ¥4750 In-stock
25 mg ¥9500 In-stock
50 mg ¥13500 In-stock
100 mg 询价

* Please select Quantity before adding items.

Ilginatinib maleate 相关产品

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生物活性

Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

IC50 & Target[1]

JAK2

0.72 nM (IC50)

Tyk2

22 nM (IC50)

JAK1

33 nM (IC50)

JAK3

39 nM (IC50)

体外研究
(In Vitro)

Ilginatinib maleate (NS-018 maleate) is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib maleate also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib maleate shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2[1].
Ilginatinib maleate (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib maleate (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ilginatinib maleate (NS-018 maleate) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model[1].
Ilginatinib maleate (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

505.50

Formula

C25H24FN7O4

CAS 号

1354799-87-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL (59.35 mM)

H2O : 1 mg/mL (1.98 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9782 mL 9.8912 mL 19.7824 mL
5 mM 0.3956 mL 1.9782 mL 3.9565 mL
10 mM 0.1978 mL 0.9891 mL 1.9782 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29.

    [2]. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

Cell Assay
[2]

Bone marrow mononuclear cells (BMMNCs) from healthy volunteers and myelodysplastic syndrome (MDS) patients are incubated in MethoCult GF H4434 methylcellulose medium containing various hematopoietic cytokines at 1.0 × 105 cells/mL with or without NS-018 at 37°C in a humidified atmosphere of 5% CO2. Commercially available purified normal human CD34-positive (CD34+) BM cells are used as a control. Burst-forming unit-erythroid (BFU-E) and colonyforming unit-granulocyte/macrophage (CFU-GM) colonies are counted under an inverted microscope on day 14 of culture[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Female BALB/c nude mice are placed in blanket cages in an environment maintained at 21-25°C and 45-65% relative humidity, with artificial illumination for 12 h and a ventilation frequency of at least 15 times/h. They are allowed free access to food pellets and tap water. Ba/F3-JAK2V617F cells (106 per mouse) are inoculated intravenously into 7-week-old mice. Administration of vehicle (0.5% methylcellulose) or Ilginatinib (NS-018) twice daily by oral gavage begins the day after cell inoculation. Survival is monitored daily, and moribund mice are humanely killed and their time of death is recorded for purposes of survival analysis. In a parallel study, all mice are humanely killed after 8 days of administration, and their spleens are removed and weighed[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29.

    [2]. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

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M2N12

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

M2N12  纯度: 98.27%

M2N12 是一种有效且高度选择性的细胞分裂周期蛋白磷酸酶 25C (Cdc25C) 抑制剂,IC50 值为 0.09 μM。 M2N12 还具有抑制 Cdc25A 和 Cdc25B 的活性,IC50 值分别为 0.53 μM 和 1.39 μM。M2N12 具有抗肿瘤活性,可用于癌症研究。

M2N12

M2N12 Chemical Structure

CAS No. : 2376577-06-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4180 In-stock
5 mg ¥3800 In-stock
10 mg ¥6000 In-stock
25 mg ¥11500 In-stock
50 mg ¥18000 In-stock
100 mg ¥28500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

M2N12 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research[1].

体外研究
(In Vitro)

M2N12 (0-20 μM; 72 hours) has cytotoxic activity against five tumor cell lines and a normal cell line including A-549, MDA-MB-231, KB, KB-VIN, MCF-7 and HBE (IC50=3.92 μM, 4.63 μM, 5.05 μM, 6.81 μM, 4.71 μM and 6.00 μM, respectively)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

393.83

Formula

C20H16ClN5O2

CAS 号

2376577-06-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 11.11 mg/mL (28.21 mM; ultrasonic and warming and heat to 67°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5392 mL 12.6958 mL 25.3917 mL
5 mM 0.5078 mL 2.5392 mL 5.0783 mL
10 mM 0.2539 mL 1.2696 mL 2.5392 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.11 mg/mL (2.82 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.11 mg/mL (2.82 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Jing L, et al. Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries. Eur J Med Chem. 2019 Sep 14;183:111696.

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JAK3-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

JAK3-IN-1  纯度: 99.98%

JAK3-IN-1 是一种有效,选择性和口服活性的 JAK3 抑制剂,IC50 为 4.8 nM。与 JAK1 (IC50 为 896 nM) 和 JAK 2 (IC50 为 1050 nM) 相比,JAK3-IN-1 对 JAK3 的选择性高 180 倍以上。

JAK3-IN-1

JAK3-IN-1 Chemical Structure

CAS No. : 1805787-93-2

规格 价格 是否有货 数量
5 mg ¥2800 In-stock
10 mg ¥4000 In-stock
50 mg ¥12000 In-stock
100 mg ¥16800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JAK3-IN-1 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM)[1].

IC50 & Target

JAK3

4.8 nM (IC50)

JAK1

896 nM (IC50)

JAK2

1050 nM (IC50)

TTK

49 nM (IC50)

BTK

794 nM (IC50)

ITK

1070 nM (IC50)

体外研究
(In Vitro)

JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM[1].
. JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC50 = 13 nM), TTK protein kinase (TTK, IC50 = 49 nM), BLK proto-oncogene (BLK, IC50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC50 = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC50s against EGFRWT and TYK2 (IC50s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC50s for BTK or ITK (IC50s = 794 and 1070 nM respectively)[1].
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM
Incubation Time: 3 hours
Result: Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.

体内研究
(In Vivo)

JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

508.02

Formula

C26H30ClN7O2

CAS 号

1805787-93-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (196.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9684 mL 9.8421 mL 19.6843 mL
5 mM 0.3937 mL 1.9684 mL 3.9369 mL
10 mM 0.1968 mL 0.9842 mL 1.9684 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.92 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

SKI V

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SKI V  纯度: 98.09%

SKI V 是一种非竞争性的,有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂,对 GST-hSK 的 IC50 为 2 μM。 SKI V 有效抑制 PI3K,对 hPI3k 的 IC50 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

SKI V

SKI V Chemical Structure

CAS No. : 24418-86-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3080 In-stock
5 mg ¥2800 In-stock
10 mg ¥4500 In-stock
50 mg ¥12500 In-stock
100 mg 询价

* Please select Quantity before adding items.

SKI V 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
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  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity[1][2].

IC50 & Target

IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)[1]

体外研究
(In Vitro)

SKI V has weak activity toward ERK2 (IC50 of 80 μM for hERK2) and does not inhibit PKC-α[1].
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis[1].
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour[2].
SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM[1].
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells[1].
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Inhibited cancer cell proliferation.

Apoptosis Analysis[1]

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Induced apoptosis.

Western Blot Analysis[2]

Cell Line: JC cells
Concentration: 0.2, 1, 5 μM
Incubation Time: Pretreated for 1 hour
Result: Decreased phospho-Akt and phospho-MEK levels.

体内研究
(In Vivo)

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells[1]
Dosage: 75 mg/kg
Administration: IP; days 1, 5, 9, 15
Result: Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

分子量

254.24

Formula

C15H10O4

CAS 号

24418-86-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (983.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9333 mL 19.6665 mL 39.3329 mL
5 mM 0.7867 mL 3.9333 mL 7.8666 mL
10 mM 0.3933 mL 1.9666 mL 3.9333 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

    [2]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务