标签归档：hydrochloride

ZM223 hydrochloride

发表于由
回复

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。

ZM223 hydrochloride  纯度: 98.93%

ZM223 hydrochloride 是一种有效的非共价 NEDD8 活化酶 (NAE) 抑制剂，具有口服活性。

ZM223 hydrochloride

ZM223 hydrochloride Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5340 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥22500 In-stock
100 mg ￥33500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ZM223 hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Ubiquitination Compound Library
  • Orally Active Compound Library
  • Targeted Diversity Library

生物活性

ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity[1].

IC50 & Target

NEDD8 activating enzyme (NAE)[1]
体外研究
(In Vitro)

ZM223 hydrochloride (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC50s of 100 and 122 nM, respectively[1].
ZM223 hydrochloride (0.1-1 μM; 4 hours) causes a dose-response decrease in the level of NEDD8 and accumulation of the UBC12 protein, indicating the decrease of the subsequent NEDD8-UBC12 complex[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: HCT116 colon cancer cells and U-2OS osteosarcoma cells
Concentration: 0.1 μM, 1 μM
Incubation Time: 4 hours
Result: Inhibited both HCT-116 and U-2OS cancer cells.

Western Blot Analysis[1]

Cell Line: HCT116 colon cancer cells
Concentration: 0.1 μM, 1 μM
Incubation Time: 4 hours
Result: Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein.

分子量

538.99

Formula

C23H18ClF3N4O2S2
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 : 150 mg/mL (278.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8553 mL 9.2766 mL 18.5532 mL
5 mM 0.3711 mL 1.8553 mL 3.7106 mL
10 mM 0.1855 mL 0.9277 mL 1.8553 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: ≥ 7.5 mg/mL (13.91 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (13.91 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 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: 7.5 mg/mL (13.91 mM); Suspended solution; Need ultrasonic

    此方案可获得 7.5 mg/mL (13.91 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 75.0 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]. Ma H, et al. Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening. Eur J Med Chem. 2017 Jun 16;133:174-183.

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

SHP2-IN-6 hydrochloride

发表于由
回复

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。

SHP2-IN-6 hydrochloride  纯度: 98.74%

SHP2-IN-6 hydrochloride 是一种有效的 SHP2 抑制剂，IC50 值为 25.8 nM，详细信息请参见专利 WO2017211303A1，compound 7。

SHP2-IN-6 hydrochloride

SHP2-IN-6 hydrochloride Chemical Structure

CAS No. : 2169223-49-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5420 In-stock
5 mg ￥4800 In-stock
10 mg ￥8000 In-stock
25 mg ￥16500 In-stock
50 mg ￥26000 In-stock
100 mg ￥40000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SHP2-IN-6 hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Phosphatase Inhibitor Library

生物活性

SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor with an IC50 of 25.8 nM. SHP2-IN-6 hydrochloride is extracted from patent WO2017211303A1, compound 7[1].

体外研究
(In Vitro)

SHP2-IN-6 inhibits the proliferation of KYSE-520 cells with an IC50 of 2.17 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

513.00

Formula

C22H27ClF2N6O2S
CAS 号

2169223-49-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°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 : 115 mg/mL (224.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9493 mL 9.7466 mL 19.4932 mL
5 mM 0.3899 mL 1.9493 mL 3.8986 mL
10 mM 0.1949 mL 0.9747 mL 1.9493 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: ≥ 5.75 mg/mL (11.21 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (11.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 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: ≥ 5.75 mg/mL (11.21 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (11.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 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
*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]. Cunbo Ma, et al. Novel heterocyclic derivatives useful as shp2 inhibitors. WO2017211303A1.

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

Pazopanib Hydrochloride(Synonyms: 盐酸帕唑帕尼; GW786034 (Hydrochloride))

发表于由
回复

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。

Pazopanib Hydrochloride (Synonyms: 盐酸帕唑帕尼; GW786034 (Hydrochloride)) 纯度: 99.84%

Pazopanib Hydrochloride (GW786034 Hydrochloride) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC50分别为10，30，47，84，74，140，146 nM。

Pazopanib Hydrochloride(Synonyms: 盐酸帕唑帕尼; GW786034 (Hydrochloride))

Pazopanib Hydrochloride Chemical Structure

CAS No. : 635702-64-6

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 ￥572 In-stock
10 mg ￥520 In-stock
50 mg ￥1100 In-stock
100 mg ￥1600 In-stock
200 mg ￥2700 In-stock
500 mg ￥4500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Pazopanib Hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Diabetes Related Compound Library
  • Anti-COVID-19 Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Therapy Drug Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

IC50 & Target[1]

VEGFR1

10 nM (IC50)

VEGFR2

30 nM (IC50)

VEGFR3

47 nM (IC50)

PDGFRβ

84 nM (IC50)

FGFR1

140 nM (IC50)

c-Kit

74 nM (IC50)

c-Fms

146 nM (IC50)

体外研究
(In Vitro)

Pazopanib shows good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50s of 84, 74, 140, and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, and monkey with low clearances (1.4-1.7 mL/min/kg) and good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, and 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 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.
体内研究
(In Vivo)

Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200−250 mm3) using HT29 (colon carcinoma), A375P (melanoma), and HN5 (head and neck carcinoma) tumors following a standard three-week course of therapy. The HN5 and HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, and the animals appeared healthy and active throughout the study duration[1]. The quantity of adherent leukocytes in the Pazopanib eye drops group is less than untreated diabetic animals and more than the healthy animals. Average leukocytes adhered to the retinal vasculature in healthy animals is 37.2±7.8, whereas diabetic animals have an average value of 102±15.6, approximately 3-fold higher than healthy animals. Animals treated with 0.5 % w/v Pazopanib suspension demonstrate 69.5±9.5 leukocytes adhered in their retinal vasculature, which is found to be significantly lower than diabetic animals[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.
Clinical Trial

分子量

473.98

Formula

C21H24ClN7O2S
CAS 号

635702-64-6
中文名称

盐酸帕唑帕尼；帕唑帕尼盐酸盐
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 : 10 mg/mL (21.10 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1098 mL 10.5490 mL 21.0979 mL
5 mM 0.4220 mL 2.1098 mL 4.2196 mL
10 mM 0.2110 mL 1.0549 mL 2.1098 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: ≥ 1 mg/mL (2.11 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.11 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (2.11 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.11 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (2.11 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.11 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 10.0 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]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640.

    [2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.
Kinase Assay
[1]

VEGFR enzyme assays are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated compound (Pazopanib) in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a plate reader[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 Assay
[1]

The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO2. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=Vmax(1−(x/(K+x))), where K is equal to the IC50[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][2]

Mice[1]
Tumors are initiated by injection of tumor cell suspension in 8−12 week old nude mice. When tumors reach a volume of 100−200 mm3, mice are randomized and divided into groups of eight. Pazopanib is administered once or twice daily at 10, 30, or 100 mg/kg. Animals are euthanized by inhalation of CO2 at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm3)=(length×width2)/2. Results are routinely reported as % inhibition=1−(average growth of the drug treated population/average growth of vehicle treated control population).
Rats[2]
Male Brown-Norway (BN; pigmented) rats weighing 200 to 250 g are acclimatized for at least two days prior to any experimental procedure. After overnight fasting for 12-16 h, an intraperitoneal injection of 30 mg/mL solution of Streptozotocin in 10 mM citrate buffer (pH 4.5) is administered (60 mg/kg body weight) to induce diabetes. After 3-4 h of Streptozotocin injection, animals are put on a regular diet and 24 h after Streptozotocin injection, blood sample (5-10 μL) is collected via tail vein. The blood glucose levels in the animals are determined with a glucose monitor. Animals with blood glucose levels greater than 250 mg/dL are considered diabetic. The animals are divided into three groups. Group 1: Healthy (n=12), Group 2: Diabetic (n=12) and Group 3: Diabetic+Treatment (n=12). Treatment is started immediately after diabetes induction. Both eyes are dosed twice daily for 30 days with 0.5 % w/v Pazopanib suspension (10 μL volume in each eye) and animals in all groups are sacrificed on day 31, 16-17 h after last dose on day 30.

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]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640.

    [2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50.

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

MMAF hydrochloride(Synonyms: Monomethylauristatin F hydrochloride)

发表于由
回复

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。

MMAF hydrochloride (Synonyms: Monomethylauristatin F hydrochloride) 纯度: 99.52%

MMAF (Monomethylauristatin F) hydrochloride 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂，用作抗肿瘤药物。MMAF hydrochloride 广泛用作抗体偶联药物 (ADCs) 的细胞毒性成分，如 Vorsetuzumab mafodotin 和 SGN-CD19A。

MMAF hydrochloride(Synonyms: Monomethylauristatin F hydrochloride)

MMAF hydrochloride Chemical Structure

CAS No. : 1415246-68-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
25 mg ￥1800 In-stock
50 mg ￥2500 In-stock
100 mg ￥3400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MMAF hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library
  • Peptidomimetic Library

生物活性

MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A[1][2][3].

IC50 & Target

Auristatin

 

体外研究
(In Vitro)

MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC50s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay[4].

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 maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[4].

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

768.42

Formula

C39H66ClN5O8
CAS 号

1415246-68-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMSO : 27 mg/mL (35.14 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3014 mL 6.5069 mL 13.0137 mL
5 mM 0.2603 mL 1.3014 mL 2.6027 mL
10 mM 0.1301 mL 0.6507 mL 1.3014 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.
Cell Assay
[1]

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[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: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[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]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

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

Lycorine hydrochloride(Synonyms: 石蒜碱)

发表于由
回复

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。

Lycorine hydrochloride (Synonyms: 石蒜碱) 纯度: 99.35%

Lycorine hydrochloride 是石蒜的主要活性成分，也是黑色素瘤血管生成抑制剂，具有抗肿瘤活性。Lycorine hydrochloride 能有效抑制 Hey1B 细胞的有丝分裂增殖 (IC50 为 1.2 μM)。

Lycorine hydrochloride(Synonyms: 石蒜碱)

Lycorine hydrochloride Chemical Structure

CAS No. : 2188-68-3

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 ￥550 In-stock
10 mg ￥500 In-stock
25 mg ￥900 In-stock
50 mg ￥1500 In-stock
100 mg ￥2200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Lycorine hydrochloride 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Autophagy Compound Library
  • Antibacterial Compound Library
  • Traditional Chinese Medicine Monomer Library
  • Alkaloids Library

生物活性

Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radia and is also a melanoma vasculogenic inhibitor and has anti-tumor activity[1]. Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM)[2].

IC50 & Target

IC50: 1.2 μM (Hey1B cells )[2]
体外研究
(In Vitro)

Lycorine hydrochloride (0-25 μM; 48 hours; C8161 cells) treatment markedly suppresses the expression of vascular endothelial (VE)-cadherin in a dose-dependent manner and also slightly diminishes the expression of Sema4D in C8161 cells. However, the expression of the other six genes is not affected[1].
Lycorine hydrochloride (0-25 μM; 48 hours; C8161 cells) treatment markedly reduces VE-cadherin protein levels in C8161 cells in a dose-dependent fashion[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.

RT-PCR[1]

Cell Line: C8161 cells
Concentration: 0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM
Incubation Time: 48 hours
Result: Markedly suppressed the expression of VE-cadherin in a dose-dependent manner and also slightly diminished the expression of Sema4D in C8161 cells.

Western Blot Analysis[1]

Cell Line: C8161 cells
Concentration: 0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM
Incubation Time: 48 hours
Result: Markedly reduced VE-cadherin protein levels in C8161 cells in a dose-dependent fashion.

体内研究
(In Vivo)

Lycorine hydrochloride (0-15 μg; subcutaneous injection; for 14 days; BALB/C nude mice) treatment has an inhibitory effect on melanoma cell-mediated tumor vasculogenic mimicry[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- to 8-week-old BALB/C nude mice[1]
Dosage: 0 μg, 7.5 μg, 15 μg
Administration: Subcutaneous injection; for 14 days
Result: Showed an inhibitory effect on melanoma cell-mediated tumor vasculogenic mimicry.

分子量

323.77

Formula

C16H18ClNO4
CAS 号

2188-68-3
中文名称

盐酸石蒜碱；石蒜碱；水仙碱
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 : 25 mg/mL (77.22 mM; Need ultrasonic)

H2O : 16.67 mg/mL (51.49 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0886 mL 15.4431 mL 30.8861 mL
5 mM 0.6177 mL 3.0886 mL 6.1772 mL
10 mM 0.3089 mL 1.5443 mL 3.0886 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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.42 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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.42 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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.42 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]. Liu, R. et al. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry. Pigment cell & melanoma research 25, 630-638, doi:10.1111/j.1755-148X.2012.01036.x (2012).

    [2]. Cao, Z. et al.Lycorine hydrochloride selectively inhibits human ovarian cancer cell proliferation and tumor neovascularization with very low toxicity. Toxicology letters 218, 174-185, doi:10.1016/j.toxlet.2013.01.018 (2013).

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

Lenampicillin-d5 hydrochloride(Synonyms: 盐酸仑氨苄西林 d5 (盐酸盐))

发表于由

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。

Lenampicillin-d5 hydrochloride (Synonyms: 盐酸仑氨苄西林 d5 (盐酸盐))

Lenampicillin-d5 hydrochloride 是 Lenampicillin hydrochloride 的氘代物。Lenampicillin hydrochloride (KBT 1585 hydrochloride) 是氨苄西林的口服前药，是一种有效的-内酰胺类抗菌(beta-lactam antibacterial) 剂，可抑制细菌的青霉素结合蛋白(转肽酶)。与氨苄西林相比，Lenampicillin 有改善吸收、减少副作用的作用，并应用于化脓性皮肤软组织感染的研究。

Lenampicillin-d5 hydrochloride(Synonyms: 盐酸仑氨苄西林 d5 (盐酸盐))

Lenampicillin-d5 hydrochloride Chemical Structure

CAS No. : 1356847-85-2

规格 是否有货
1 mg Check price and availability
5 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Lenampicillin-d5 (KBT 1585-d5) hydrochloride is the deuterium labeled Lenampicillin hydrochloride. Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.98

Formula

C21H19D5ClN3O7S
CAS 号

1356847-85-2
中文名称

盐酸仑氨苄西林 d5 (盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. FUMIO OGINO, et al. ACUTE TOXICITY OF LENAMPICILLIN HYDROCHLORIDE (KBT-1585) IN MICE, RATS AND DOGS

    [3]. Yamabe S, et al. Non-mutagenicity of KBT-1585, a novel ester of ampicillin.Chemioterapia. 1984 Feb;3(1):60-2.

    [4]. Fujita K, et al. Clinical evaluation of lenampicillin in the treatment of superficial suppurative skin and soft tissue infection. A double-blind study comparing amoxicillin.Jpn J Antibiot. 1985 Jul;38(7):1794-818.

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

Abemaciclib metabolite M18 hydrochloride(Synonyms: LSN3106729 hydrochloride)

发表于由

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。

Abemaciclib metabolite M18 hydrochloride (Synonyms: LSN3106729 hydrochloride) 纯度: 99.01%

Abemaciclib metabolite M18 (LSN3106729) hydrochloride，Abemaciclib 的代谢物，是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 hydrochloride 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18 hydrochloride(Synonyms: LSN3106729 hydrochloride)

Abemaciclib metabolite M18 hydrochloride Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4090 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Abemaciclib metabolite M18 hydrochloride 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-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

531.00

Formula

C25H29ClF2N8O
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 : 125 mg/mL (235.40 mM; Need ultrasonic)

H2O : 100 mg/mL (188.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8832 mL 9.4162 mL 18.8324 mL
5 mM 0.3766 mL 1.8832 mL 3.7665 mL
10 mM 0.1883 mL 0.9416 mL 1.8832 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。
参考文献

  • [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

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

Irinotecan-d10 hydrochloride(Synonyms: 伊立替康 d10 (盐酸盐))

发表于由

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。

Irinotecan-d10 hydrochloride (Synonyms: 伊立替康 d10 (盐酸盐))

Irinotecan-d10 hydrochloride 是 Irinotecan 的氘代物。Irinotecan ((+)-Irinotecan) 是一种拓扑异构酶 I (topoisomerase I) 抑制剂，可用于结肠癌和直肠癌的研究。

Irinotecan-d10 hydrochloride(Synonyms: 伊立替康 d10 (盐酸盐))

Irinotecan-d10 hydrochloride Chemical Structure

CAS No. : 718612-62-5

规格 价格 是否有货
1 mg ￥8100 询问价格 & 货期
5 mg ￥24000 询问价格 & 货期
10 mg ￥39000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Irinotecan-d10 ((+)-Irinotecan-d10) hydrochloride is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

633.20

Formula

C33H29D10ClN4O6
CAS 号

718612-62-5
中文名称

伊立替康 d10 (盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26.

    [3]. Pavillard V, et al. Determinants of the cytotoxicity of irinotecan in two human colorectal tumor cell lines. Cancer Chemother Pharmacol. 2002 Apr;49(4):329-35. Epub 2002 Jan 30.

    [4]. Allegrini G, et al. Thrombospondin-1 plus irinotecan: a novel antiangiogenic-chemotherapeutic combination that inhibits the growth of advanced human colon tumor xenografts in mice. Cancer Chemother Pharmacol. 2004 Mar;53(3):261-6. Epub 2003 Dec 5.

    [5]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116.

    [6]. Huang MY, et al. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis. Apoptosis. 2016 Feb;21(2):130-42.

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

Pirarubicin Hydrochloride(Synonyms: 盐酸吡柔比星; THP Hydrochloride)

发表于由

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。

Pirarubicin Hydrochloride (Synonyms: 盐酸吡柔比星; THP Hydrochloride) 纯度: 98.51%

Pirarubicin Hydrochloride (THP Hydrochloride) 是一种蒽环类抗生素，为拓扑异构酶 II (topoisomerase II) 的抑制剂，可用于各种癌症尤其是实体瘤的研究。

Pirarubicin Hydrochloride(Synonyms: 盐酸吡柔比星; THP Hydrochloride)

Pirarubicin Hydrochloride Chemical Structure

CAS No. : 95343-20-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605 In-stock
10 mg ￥550 In-stock
50 mg ￥2100 In-stock
100 mg ￥3720 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Pirarubicin Hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Natural Product Like Compound Library
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Antibacterial Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • FDA Approved & Pharmacopeial Drug Library
  • Antibiotics Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.

IC50 & Target

Topoisomerase II

 

体外研究
(In Vitro)

Pirarubicin is a topoisomerase II inhibitor[1]. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells, with IC50s of 0.366 and 0.078 μM, respectively. The cytotoxicity of Pirarubicin toward M5076 cells is lower than toward Ehrlich cells, and this is due to the much lower expression of topoisomerase II in M5076 cells than in Ehrlich cells[2]. Pirarubicin (2.5, 5, 10 μg/mL) significantly induces autophagy in a dose dependent manner in bladder cancer (T24, EJ, 5637, J82 and UM-UC-3) cells. Furthmore, Pirarubicin (5 μg/mL) induces apoptosis through inhibition of mTOR/p70S6K/4E-BP1 in bladder cancer cells, and this effect is enhanced by inhibition of autophagy[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)

Pirarubicin (18 mg/kg, i.v.) significantly elevates serum level of BNP, CK-MB, CTnT, LDH, and MDA compared with those in the control group in acute cardiac toxicity rats. Pirarubicin also lowers heart rate, and depresses R-wave voltage, and prolongation of QT intervals in the acute cardiac toxicity model[4].

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

664.10

Formula

C32H38ClNO12
CAS 号

95343-20-7
中文名称

盐酸吡柔比星；盐酸吡喃阿霉素；盐酸吡柔吡星
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 : 20.83 mg/mL (31.37 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5058 mL 7.5290 mL 15.0580 mL
5 mM 0.3012 mL 1.5058 mL 3.0116 mL
10 mM 0.1506 mL 0.7529 mL 1.5058 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: ≥ 2.08 mg/mL (3.13 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.13 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

*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]. Takigawa N, et al. Cytotoxic effect of topoisomerase II inhibitors against adriamycin- and etoposide-resistant small cell lung cancer sublines. Gan To Kagaku Ryoho. 1993 May;20(7):929-35.

    [2]. Nagai K, et al. Relationships between the in vitro cytotoxicity and transport characteristics of pirarubicin and doxorubicin in M5076 ovarian sarcoma cells, and comparison with those in Ehrlich ascites carcinoma cells. Cancer Chemother Pharmacol. 2002 Mar;49(3):244-50. Epub 2002 Jan 8.

    [3]. Li K, et al. Pirarubicin induces an autophagic cytoprotective response through suppression of the mammalian target of rapamycin signaling pathway in human bladder cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):380-5.

    [4]. Wang YD, et al. Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity. J Asian Nat Prod Res. 2017 Oct 27:1-13.
Cell Assay
[3]

MTS is used to analyze cell survival. Briefly, cells are plated in 96-well plates in triplicate at 2 × 103 cells per well and cultured in growth medium. Then cells are treated with pirarubicin at different concentrations (2.5 μg/mL, 5 μg/mL, 10 μg/mL) for 24 h. MTS reagent (5 mg/mL) is added and incubated at 37°C for 4 h. The absorbance is monitored at 490 nm using a microplate reader[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.
Animal Administration
[4]

An acute cardiac toxicity model is established by a single dose of 18 mg/kg pirarubicin through the caudal vein injection. Thirty-six rats are randomized equally to six groups: normal control, cardiac injury (THP) model, dexrazoxane (180 mg/kg), low-dose rutin (25 mg/kg), middle-dose rutin (50 mg/kg), and high-dose rutin (100 mg/kg). Rats in the rutin-treated group are administered different doses of rutin and CMC-Na for 7 days by gavage and a single dose of 18 mg/kg pirarubicin through caudal vein injection. Rats in the dexrazoxane-treated group receive sodium carboxymethylcellulose (CMC-Na) by gavage for six days. 40 mg/kg dexrazoxane is then administered to rats by intraperitoneal injection and 18 mg/kg pirarubicin is administered by caudal vein injection on day 7. Rats in the THP model group receive CMC-Na by gavage for seven days, followed by pirarubicin 18 mg/kg through the caudal vein injection on day 7. Rats in the normal control group receive CMC-Na by gavage for seven days, followed by saline through caudal vein injection on day 7[4].

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]. Takigawa N, et al. Cytotoxic effect of topoisomerase II inhibitors against adriamycin- and etoposide-resistant small cell lung cancer sublines. Gan To Kagaku Ryoho. 1993 May;20(7):929-35.

    [2]. Nagai K, et al. Relationships between the in vitro cytotoxicity and transport characteristics of pirarubicin and doxorubicin in M5076 ovarian sarcoma cells, and comparison with those in Ehrlich ascites carcinoma cells. Cancer Chemother Pharmacol. 2002 Mar;49(3):244-50. Epub 2002 Jan 8.

    [3]. Li K, et al. Pirarubicin induces an autophagic cytoprotective response through suppression of the mammalian target of rapamycin signaling pathway in human bladder cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):380-5.

    [4]. Wang YD, et al. Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity. J Asian Nat Prod Res. 2017 Oct 27:1-13.

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

Dimethylamine-d6 hydrochloride

发表于由

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。

Dimethylamine-d6 hydrochloride  纯度: ≥99.0%

Dimethylamine-d6 hydrochloride 是一种氘代标记的 Dimethylamine hydrochloride。Dimethylamine hydrochloride 是二甲基亚硝胺的直接前体，二甲基亚硝胺是一种已知的多种动物体内的强效致癌物。

Dimethylamine-d6 hydrochloride

Dimethylamine-d6 hydrochloride Chemical Structure

CAS No. : 53170-19-7

规格 价格 是否有货 数量
25 mg ￥500 In-stock
50 mg ￥800 In-stock
100 mg ￥1300 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Dimethylamine-d6 hydrochloride is a deuterium labeled Dimethylamine hydrochloride. Dimethylamine hydrochloride is the immediate precursor of dimethylnitrosamine, a known potent carcinogen in a wide variety of animal species[1].

分子量

87.58

Formula

C2H2D6ClN
CAS 号

53170-19-7
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
参考文献

  • [1]. Zhang AQ, et al. Dimethylamine formation in the rat from various related amine precursors. Food Chem Toxicol. 1998;36(11):923-927.

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

Trilaciclib hydrochloride(Synonyms: G1T28 hydrochloride)

发表于由

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。

Trilaciclib hydrochloride (Synonyms: G1T28 hydrochloride) 纯度: 99.24%

Trilaciclib hydrochloride (G1T28 hydrochloride) 是 CDK4/6 的抑制剂，对 CDK4 和 CDK6 的 IC50 值分别为 1 nM 和 4 nM。

Trilaciclib hydrochloride(Synonyms: G1T28 hydrochloride)

Trilaciclib hydrochloride Chemical Structure

CAS No. : 1977495-97-8

规格 价格 是否有货 数量
1 mg ￥500 In-stock
5 mg ￥1400 In-stock
10 mg ￥2000 In-stock
50 mg ￥6400 In-stock
100 mg ￥9900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Trilaciclib hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively[1].

IC50 & Target

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

体外研究
(In Vitro)

Incubation with Trilaciclib hydrochloride (G1T28) for 24 hours induces a robust G1 cell-cycle arrest (time=0). By 16 hours after Trilaciclib hydrochloride washout, cells have reentered the cell cycle and demonstrate cell-cycle kinetics similar to untreated control cells. These results demonstrate that Trilaciclib hydrochloride causes a transient, and reversible G1 arrest. A transient Trilaciclib hydrochloride-mediated G1 cell-cycle arrest in CDK4/6-sensitive cells decreases the in vitro toxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression[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)

Trilaciclib hydrochloride (G1T28) treatment results in a robust and dose-dependent suppression of proliferation in HSPCs at 12 hours, with 5-ethynyl-2′-deoxyuridine (EdU) incorporation returning near baseline levels in a dose-dependent manner by 24 hours after administration. These data demonstrate that a single oral dose of Trilaciclib hydrochloride can produce reversible cell-cycle arrest in HSPCs in a dose-dependent manner in vivo. Mice given 100 mg/kg Trilaciclib hydrochloride 30 minutes prior to etoposide treatment, exhibits only background levels of caspase-3/7 activity. These data demonstrate that Trilaciclib hydrochloride can protect the bone marrow from chemotherapy-induced apoptosis in vivo. The data demonstrate that treatment with Trilaciclib hydrochloride prior to 5-fluorouracil (5-FU) likely decreases 5-FU-induced damage by chemotherapy in HSPCs, thus accelerating blood count recovery after chemotherapy[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

519.47

Formula

C24H32Cl2N8O
CAS 号

1977495-97-8
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: 

H2O : 25.64 mg/mL (49.36 mM; ultrasonic and adjust pH to 2 with HCl)

DMSO : 1.1 mg/mL (2.12 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9250 mL 9.6252 mL 19.2504 mL
5 mM 0.3850 mL 1.9250 mL 3.8501 mL
10 mM 0.1925 mL 0.9625 mL 1.9250 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。
参考文献

  • [1]. Bisi JE, et al. Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93.
Kinase Assay
[1]

HS68, WM2664, and A2058 cells are treated with 300 nM Trilaciclib hydrochloride (G1T28) or DMSO (0.1%), for 4, 8, 16, or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the kit, according to the manufacturer’s instructions. For Western blot analysis, protein is processed as described previously. Antibodies to total RB and β-tubulin run as a loading control are assessed[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 Assay
[1]

HS68 cells are treated for 24 hours with Trilaciclib hydrochloride (G1T28) at 10, 30, 100, 300, 1,000, or 3,000 nM final concentration. Cells are harvested and fixed in ice-cold methanol. Fixed cells are stained with 20 μg propidium iodide, 50 μg RNAse A in PBS-CMF (calcium magnesium free) +1% BSA, Fraction V. Samples are processed on Cyan ADP Analyzer, and cell-cycle analysis is completed using software[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]

Female athymic nude mice are implanted with H69 cells and monitored until treatment initiation. Once tumors reach an acceptable size (150 mm3), mice are dosed in various combinations of Trilaciclib hydrochloride (G1T28) and topotecan for 5 days per week for 4 weeks. Tumors are measured for up to 60 days after treatment. All mice that reach excessive tumor burden before 60 days are humanely euthanized. Topotecan and Trilaciclib hydrochloride levels in blood plasma from the mice treated with Trilaciclib hydrochloride and/or topotecan are processed and analyzed using established methods[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]. Bisi JE, et al. Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93.

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

L-Buthionine-(S,R)-sulfoximine hydrochloride(Synonyms: L-Buthionine sulfoximine hydrochloride; L-BSO hydrochloride)

发表于由

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。

L-Buthionine-(S,R)-sulfoximine hydrochloride (Synonyms: L-Buthionine sulfoximine hydrochloride; L-BSO hydrochloride)

L-Buthionine-(S,R)-sulfoximine hydrochloride 是一种具有细胞渗透性的、有效的、快速起效的、具有口服活性的、不可逆的 G-谷氨酸半胱氨酸合成酶 (γ-glutamylcysteine synthetase) 抑制剂，可降低细胞内谷胱甘肽的水平，其对黑色素瘤、乳腺卵巢癌标本的 IC50 值分别为1.9 μM、8.6 μM 和29 μM。

L-Buthionine-(S,R)-sulfoximine hydrochloride(Synonyms: L-Buthionine sulfoximine hydrochloride; L-BSO hydrochloride)

L-Buthionine-(S,R)-sulfoximine hydrochloride Chemical Structure

规格 价格 是否有货
10 mM * 1 mL in DMSO ￥660 询问价格 & 货期
50 mg ￥600 询问价格 & 货期

* Please select Quantity before adding items.

L-Buthionine-(S,R)-sulfoximine hydrochloride 的其他形式现货产品:

DL-Buthionine-(S,R)-sulfoximine L-Buthionine-(S,R)-sulfoximine

L-Buthionine-(S,R)-sulfoximine hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library

生物活性

L-Buthionine-(S,R)-sulfoximine hydrochloride is a cell-permeable, potent, fast acting, orally active and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively[1][2].

体外研究
(In Vitro)

L-Buthionine-(S,R)-sulfoximine (BSO: 50 μM) treatment for 48 hr results in a 95% decrease in ZAZ and M14 melanoma cell line GSH levels, and a 60% decrease in GST enzyme activity. GST-π protein and mRNA levels are significantly reduced in both cell lines[1]. L-Buthionine-(S,R)-sulfoximine (BSO) induces oxidative stress in a cell by irreversibly inhibiting g-glutamylcysteine synthetase, an essential enzyme for the synthesis of glutathione (GSH)[2].
L-Buthionine-(S,R)-sulfoximine (BSO) induces ferroptosis in cancer cells[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)

BSO causes an elevated frequency of DNA deletions during mouse development. BSO treatment reduced GSH concentration in mouse fetuses by 55% and 70% at 2 mM and 20 mM BSO doses, respectively, compared to untreated mice. Co-treatment with 2 mM BSO and 20 mM NAC depleted GSH to a similar extent as 2 mM BSO, consistent with the function of BSO to inhibit the g-GCS enzyme indispensable for GSH synthesis. Like GSH, cysteine levels dropped following BSO treatment[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

258.77

Formula

C8H19ClN2O3S
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 : 250 mg/mL (966.11 mM; Need ultrasonic)

H2O : 100 mg/mL (386.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8644 mL 19.3222 mL 38.6444 mL
5 mM 0.7729 mL 3.8644 mL 7.7289 mL
10 mM 0.3864 mL 1.9322 mL 3.8644 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 (8.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.04 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 (8.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.04 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 (8.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.04 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]. Fruehauf JP, et al. Selective and synergistic activity of L-S,R-buthionine sulfoximine on malignant melanoma is accompanied by decreased expression of glutathione-S-transferase. Pigment Cell Res. 1997 Aug;10(4):236-49.

    [2]. Reliene R, et al. Glutathione depletion by buthionine sulfoximine induces DNA deletions in mice. Carcinogenesis. 2006 Feb;27(2):240-4.

    [3]. Satoru Nishizawa, et al. Low tumor glutathione level as a sensitivity marker for glutamate-cysteine ligase inhibitors. Oncol Lett. 2018 Jun;15(6):8735-8743.

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

PIK-75 hydrochloride

发表于由

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。

PIK-75 hydrochloride  纯度: 99.72%

PIK-75 hydrochloride 是一种可逆的 DNA-PK 和 p110α-选择性的抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC50 分别为 2，5.8 和 76 nM。PIK-75 hydrochloride 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。PIK-75 hydrochloride 诱导凋亡 (apoptosis)。

PIK-75 hydrochloride

PIK-75 hydrochloride Chemical Structure

CAS No. : 372196-77-5

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 ￥563 In-stock
10 mg ￥512 In-stock
50 mg ￥2232 In-stock
100 mg ￥2727 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PIK-75 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage 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
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 hydrochloride induces apoptosis[3].

IC50 & Target[1]

DNA-PK

2 nM (IC50)

p110α

5.8 nM (IC50)

p110γ

76 nM (IC50)

p110δ

510 nM (IC50)

p110β

1.3 μM (IC50)

hsVPS34

2.6 μM (IC50)

PI3KC2β

1 μM (IC50)

PI3KC2α

10 μM (IC50)

mTORC1

1 μM (IC50)

mTORC2

10 μM (IC50)

ATM

2.3 μM (IC50)

ATR

21 μM (IC50)

PI4KIIIβ

50 μM (IC50)

体外研究
(In Vitro)

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively[1].
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells[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.

Cell Viability Assay[3]

Cell Line: Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time: 48 hours
Result: Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.

Western Blot Analysis[2]

Cell Line: Overnight-starved CHO-IR cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 5 minutes
Result: Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner.

体内研究
(In Vivo)

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice[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.

Animal Model: Mice bearing tumors of MIA PaCa-2[3]
Dosage: 2 mg/kg; or combination with Gemcitabine (20 mg/kg)
Administration: Administered injection; 5 times per week. 25 days
Result: Reduced the tumor growth and enhanced the antitumor effect.

分子量

488.74

Formula

C16H15BrClN5O4S
CAS 号

372196-77-5
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 : 11 mg/mL (22.51 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0461 mL 10.2304 mL 20.4608 mL
5 mM 0.4092 mL 2.0461 mL 4.0922 mL
10 mM 0.2046 mL 1.0230 mL 2.0461 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: ≥ 1.1 mg/mL (2.25 mM); Clear solution

    此方案可获得 ≥ 1.1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 11.0 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: ≥ 1.1 mg/mL (2.25 mM); Clear solution

    此方案可获得 ≥ 1.1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 11.0 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: ≥ 1.1 mg/mL (2.25 mM); Clear solution

    此方案可获得 ≥ 1.1 mg/mL (2.25 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 11.0 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]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

    [2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58.

    [3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69.

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

GSK-J4 hydrochloride

发表于由

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。

GSK-J4 hydrochloride  纯度: 98.83%

GSK-J4 hydrochloride 是一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC50 分别为 8.6 μM 和 6.6 μM。GSK-J4 hydrochloride 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50 值为 9 μM。GSK-J4 hydrochloride 是 GSK-J1 的细胞通透性前药。

GSK-J4 hydrochloride

GSK-J4 hydrochloride Chemical Structure

CAS No. : 1797983-09-5

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 ￥1320 In-stock
10 mg ￥1200 In-stock
50 mg ￥4500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

GSK-J4 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library

生物活性

GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1[1][2][3].

IC50 & Target

IC50: 8.6 µM (JMJD3/KDM6B), 6.6 µM (UTX/KDM6A)[6]
体外研究
(In Vitro)

GSK-J4 Hydrochloride has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α)[1].
GSK-J4 Hydrochloride (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels[2].
GSK-J4 Hydrochloride (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells[3].
GSK-J4 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1[4].
GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[5].

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)

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice[2].
GSK-J4 Hydrochloride (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[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.

Animal Model: Eight-week-old male db/m and db/db mice on a BKS background[2]
Dosage: 10 mg/kg
Administration: i.p.; thrice-weekly for 10 weeks
Result: Attenuated the development of kidney disease in diabetic mice.

分子量

453.96

Formula

C24H28ClN5O2
CAS 号

1797983-09-5
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 : 62.5 mg/mL (137.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2028 mL 11.0142 mL 22.0284 mL
5 mM 0.4406 mL 2.2028 mL 4.4057 mL
10 mM 0.2203 mL 1.1014 mL 2.2028 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 (4.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.58 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 (4.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.58 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]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.

    [2]. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499.

    [3]. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117.

    [4]. Yapp C, et al. H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis. Arthritis Res Ther. 2016 Jul 7;18(1):158

    [5]. Kamikawa YF, et al. Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cells. PLoS One. 2015 May 20;10(5):e0125626

    [6]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2

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

Leelamine-d4 hydrochloride

发表于由

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。

Leelamine-d4 hydrochloride 

Leelamine-d4 hydrochloride 是 Leelamine hydrochloride 的氘代物。Leelamine hydrochloride 是一种从松树皮中提取的三环二萜分子。Leelamine hydrochloride 是一种大麻素 1 型 (CB1) 激动剂，也是前列腺癌细胞中 SREBP1 调节的脂肪酸/脂质合成的抑制剂，不受雄激素受体状态的影响。Leelamine hydrochloride 抑制调节脂肪酸合成的雄激素受体 (androgen receptor) 的转录活性。

Leelamine-d4 hydrochloride

Leelamine-d4 hydrochloride Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Leelamine-d4 hydrochloride is the deuterium labeled Leelamine hydrochloride. Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees[1]. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

325.95

Formula

C20H28D4ClN
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kuzu OF, et al. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014 Jul;13(7):1690-703.

    [3]. A.O. Ibegbu, et al. Therapeutic Potentials and uses of Cannabinoid Agonists in Health and Disease Conditions. British Journal of Pharmacology and Toxicology 3(2): 76-88, 2012

    [4]. Singh KB, et al. Leelamine is a Novel Lipogenesis Inhibitor in Prostate Cancer Cells In Vitro and In Vivo. Mol Cancer Ther. 2019 Aug 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

Heme Oxygenase-1-IN-1 hydrochloride

发表于由

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。

Heme Oxygenase-1-IN-1 hydrochloride  纯度: 99.03%

Heme Oxygenase-1-IN-1 hydrochloride (Compound 2) 是血红素加氧酶 1 (HO-1) 抑制剂，IC50 为 250 nM。

Heme Oxygenase-1-IN-1 hydrochloride

Heme Oxygenase-1-IN-1 hydrochloride Chemical Structure

CAS No. : 1092851-70-1

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 ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
50 mg ￥14000 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Heme Oxygenase-1-IN-1 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Mitochondria-Targeted Compound Library

生物活性

Heme Oxygenase-1-IN-1 hydrochloride (Compound 2) is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 250 nM[1].

分子量

315.64

Formula

C13H16BrClN2
CAS 号

1092851-70-1
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 : 125 mg/mL (396.02 mM; Need ultrasonic)

H2O : 100 mg/mL (316.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1682 mL 15.8408 mL 31.6817 mL
5 mM 0.6336 mL 3.1682 mL 6.3363 mL
10 mM 0.3168 mL 1.5841 mL 3.1682 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 (6.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.59 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 (6.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.59 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 (6.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.59 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]. Floresta G, et al. Development of new HO-1 inhibitors by a thorough scaffold-hopping analysis. Bioorg Chem. 2018 Dec;81:334-339.

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

ML241 hydrochloride

发表于由

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。

ML241 hydrochloride  纯度: 99.78%

ML241 hydrochloride 是一种有效的 p97 抑制剂，IC50 值为 100 nM。

ML241 hydrochloride

ML241 hydrochloride Chemical Structure

CAS No. : 2070015-13-1

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 ￥880 In-stock
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
25 mg ￥2900 In-stock
50 mg ￥5000 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ML241 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Anti-Aging Compound Library
  • Ubiquitination Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Targeted Diversity Library

生物活性

ML241 hydrochloride is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.

IC50 & Target

IC50: 100 nM (p97)[1]
体外研究
(In Vitro)

ML241 hydrochloride is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 values of 100 nM. ML241 inhibits p97 competitively with respect to ATP with a Ki values of 0.35 μM. ML241 (20 μM) shows no obvious inhibition of the appr 170 kinases tested. ML241 stabilizes UbG76V-GFP with IC50 of 3.5 μM[1]. ML241 is cytotoxic to HCT15 and SW403 cells, with GI50s of 53 and 33 μM after treatment for 24 h, and 13 and 12 μM after treatment for 72 h, respectively[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

408.92

Formula

C23H25ClN4O
CAS 号

2070015-13-1
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 : ≥ 34 mg/mL (83.15 mM)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” 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 2.4455 mL 12.2273 mL 24.4547 mL
5 mM 0.4891 mL 2.4455 mL 4.8909 mL
10 mM 0.2445 mL 1.2227 mL 2.4455 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 (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 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 (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 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 (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 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]. Chou TF, et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem. 2013 Feb;8(2):297-312.

    [2]. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April 14, 2011.
Cell Assay
[2]

HeLa cells stably expressing ODD-luciferase are seeded onto a 96-well white solid bottom plate (5000 cells/well) and cells are grown for 16 h. Cells are treated with DMEM containing MG132 (4 μM) for 1h and washed with 100 μL PBS twice. DMEM containing 2.5% FBS, cycloheximide (50 μg/mL) and ML241 are added into the well. Four 96-well plates are prepared and one of the plates is taken out from incubator at each time point (70, 90, 120, or 150 min). Luciferin (50 μL of 1 mg/mL in PBS) is added into each well containing 50 μL of medium and incubated at room temperature with shaking at 500 rpm for 5 min. Luminescence intensity is determined with 0.1 ms integration time on the Synergy HT Microplate Reader[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.
参考文献

  • [1]. Chou TF, et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem. 2013 Feb;8(2):297-312.

    [2]. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April 14, 2011.

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

Epertinib hydrochloride(Synonyms: S-22611 hydrochloride)

发表于由

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。

Epertinib hydrochloride (Synonyms: S-22611 hydrochloride) 纯度: 99.76%

Epertinib hydrochloride (S-22611 hydrochloride) 是一种有效，可口服，可逆的，选择性的 EGFR，HER2 和 HER4 抑制剂，IC50 值分别为 1.48 nM，7.15 nM 和 2.49 nM。Epertinib hydrochloride 具有高效的抗肿瘤活性。

Epertinib hydrochloride(Synonyms: S-22611 hydrochloride)

Epertinib hydrochloride Chemical Structure

CAS No. : 2071195-74-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3412 In-stock
5 mg ￥2600 In-stock
10 mg ￥4200 In-stock
25 mg ￥7600 In-stock
50 mg ￥12000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Epertinib hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer 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

Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1].

IC50 & Target[1]

EGFR

1.48 nM (IC50)

HER4

2.49 nM (IC50)

HER2

7.15 nM (IC50)

分子量

596.48

Formula

C30H28Cl2FN5O3
CAS 号

2071195-74-7
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 : 125 mg/mL (209.56 mM; Need ultrasonic)

H2O : 33.33 mg/mL (55.88 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6765 mL 8.3825 mL 16.7650 mL
5 mM 0.3353 mL 1.6765 mL 3.3530 mL
10 mM 0.1677 mL 0.8383 mL 1.6765 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 (3.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 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 (3.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 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]. [1]. Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8.

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

Buformin-d9 hydrochloride(Synonyms: 1-Butylbiguanide-d9 hydrochloride)

发表于由

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。

Buformin-d9 hydrochloride (Synonyms: 1-Butylbiguanide-d9 hydrochloride)

Buformin-d9 (1-Butylbiguanide-d9) hydrochloride 是 Buformin 的氘代物。Buformin (1-Butylbiguanide) 是一种有效的 AMPK 活化剂，也是具有口服活性的双胍类降血糖试剂 (antidiabetic agent)。Buformin 降低肝糖异生并降低血糖生成。Buformin 也具有抗癌活性，可以应用于癌症研究，如宫颈癌、乳腺癌等。

Buformin-d9 hydrochloride(Synonyms: 1-Butylbiguanide-d9 hydrochloride)

Buformin-d9 hydrochloride Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Buformin-d9 (1-Butylbiguanide-d9) hydrochloride is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

202.73

Formula

C6H7D9ClN5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Amanda B Parris, et al. Buformin Inhibits the Stemness of erbB-2-overexpressing Breast Cancer Cells and Premalignant Mammary Tissues of MMTV-erbB-2 Transgenic Mice. J Exp Clin Cancer Res

    [3]. Jing Li, et al. Buformin Suppresses Proliferation and Invasion via AMPK/S6 Pathway in Cervical Cancer and Synergizes With Paclitaxel. Cancer Biol Ther. 2018 Jun 3;19(6):507-517.

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

Amiselimod hydrochloride(Synonyms: MT-1303 hydrochloride)

发表于由

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。

Amiselimod hydrochloride (Synonyms: MT-1303 hydrochloride) 纯度: 99.01%

Amiselimod hydrochloride 是一个新颖的S1P1受体的调节剂。

Amiselimod hydrochloride(Synonyms: MT-1303 hydrochloride)

Amiselimod hydrochloride Chemical Structure

CAS No. : 942398-84-7

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 ￥1100 In-stock
5 mg ￥1000 In-stock
10 mg ￥1500 In-stock
25 mg ￥2500 In-stock
50 mg ￥4500 In-stock
100 mg ￥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Amiselimod hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • Orally Active Compound Library
  • Rare Diseases Drug Library

生物活性

Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. target: S1P1 In vivo: After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1 , high selectivity for S1P5 , minimal agonist activity for S1P4 , no distinct agonist activity for S1P2 or S1P3 , and approximately 5-fold weaker GIRK activation than fingolimod-P. [1] Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions. [2]

Clinical Trial

分子量

413.90

Formula

C19H31ClF3NO3
CAS 号

942398-84-7
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 : 110 mg/mL (265.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4160 mL 12.0802 mL 24.1604 mL
5 mM 0.4832 mL 2.4160 mL 4.8321 mL
10 mM 0.2416 mL 1.2080 mL 2.4160 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: ≥ 2.75 mg/mL (6.64 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (6.64 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
  • 2.

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

    Solubility: ≥ 2.75 mg/mL (6.64 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (6.64 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]. Sugahara K et al. Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk. Br J Pharmacol. 2016 Oct 7.

    [2]. Kappos L et al. Safety and efficacy of amiselimod in relapsing multiple sclerosis (MOMENTUM): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Neurol. 2016 Oct;15(11):1148-59.

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