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Cerdulatinib hydrochloride(Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

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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。

Cerdulatinib hydrochloride (Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride) 纯度: 99.54%

Cerdulatinib hydrochloride (PRT062070) 是一种选择性，具有口服活性和可逆的 ATP 竞争性的 SYK 和 JAK 的双重抑制剂，抑制 SYK 和 Tyk2、JAK1、2、3 的 IC50 值分别为 32 nM、0.5 nM、12 nM、6 nM 和 8 nM。Cerdulatinib hydrochloride 可用于研究自身免疫性疾病和B细胞恶性肿瘤。

Cerdulatinib hydrochloride(Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

Cerdulatinib hydrochloride Chemical Structure

CAS No. : 1369761-01-2

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 ￥1150 In-stock
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
50 mg ￥3600 In-stock
100 mg ￥6200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Cerdulatinib 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
  • Protein Tyrosine Kinase Compound 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
  • 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
  • Rare Diseases Drug Library

生物活性

Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies[1][2].

IC50 & Target

Tyk2

0.5 nM (IC50)

JAK1

12 nM (IC50)

JAK2

6 nM (IC50)

JAK3

8 nM (IC50)

SYK

32 nM (IC50)

MST1

4 nM (IC50)

ARK5

4 nM (IC50)

MLK1

5 nM (IC50)

FMS

5 nM (IC50)

AMPK

6 nM (IC50)

TBK1

10 nM (IC50)

MARK1

10 nM (IC50)

PAR1B-a

13 nM (IC50)

TSSK

14 nM (IC50)

MST2

15 nM (IC50)

GCK

18 nM (IC50)

JNK3

18 nM (IC50)

Rsk2

20 nM (IC50)

Rsk4

28 nM (IC50)

CHK1

42 nM (IC50)

Flt4

51 nM (IC50)

Flt3

90 nM (IC50)

Ret

105 nM (IC50)

Itk

194 nM (IC50)

体外研究
(In Vitro)

Cerdulatinib (0.03-4 μM) inhibits ERK Y204 phosphorylation with an IC50 of 0.5 μM and reduces the ability to upregulate cellsurface expression of the early activation marker CD69 with an IC50 of 0.11 μM in B cells in human whole blood[1].
Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC50 of 0.12 μM[1].
Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways[1].
Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition[1].
Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines[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: SU-DHL4; SU-DHL6; Ramosand and Daudi cells
Concentration: 0, 1, 3 μM
Incubation Time: 48 hours
Result: Inhibits cells viability with the IC50s of 0.73-1.39 μM.

Apoptosis Analysis[1]

Cell Line: SU-DHL4, SU-DHL6, and Ramos cells
Concentration: 0, 1.6, 5.0, 15 μM
Incubation Time: 72 hours
Result: Induced SU-DHL4, SU-DHL6, and Ramos cells apoptosis.

体内研究
(In Vivo)

Cerdulatinib (0.5-5 mg/kg; twice daily p.o. for 2 weeks) elicits dose-dependent efficacy in the rat collagen-induced arthritis (CIA) model[1].
Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in 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.

Animal Model: Female Lewis rats (7-8 weeks old; 159-187 g) are immunized[1]
Dosage: 0, 0.5, 1.5, 3, 5 mg/kg
Administration: Oral gavage twice daily for 2 weeks
Result: Modulated inflammation in the rat CIA treatment model.
Affected anticollagen antibody formation.
Animal Model: Balb/c mice are received BCR stimulation[1]
Dosage: 0, 1, 5, 15, 20, 30 mg/kg
Administration: Oral gavage twice daily for 5 days
Result: Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%.
Inhibited mouse splenomegaly in a dose- and concentration-dependent manner.

Clinical Trial

分子量

482.00

Formula

C20H28ClN7O3S
CAS 号

1369761-01-2
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 : 20 mg/mL (41.49 mM; ultrasonic and warming and heat to 80°C)

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 2.0747 mL 10.3734 mL 20.7469 mL
5 mM 0.4149 mL 2.0747 mL 4.1494 mL
10 mM 0.2075 mL 1.0373 mL 2.0747 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 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (4.15 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 20.0 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]. Coffey G, et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec; 351(3): 538-48.

    [2]. Ishikawa C, et, al. Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor. Int J Oncol. 2018 Oct; 53(4): 1681-1690.

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Silver Nanowire, conductive, diameter 80 nm, length, 50 microns Cat. No. SNW-01-1 80 nm 1 mL修饰性聚乙二醇

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上海金畔生物科技有限公司提供各种分子量和基团修饰性聚乙二醇定制服务。

Silver Nanowire, conductive, diameter 80 nm, length, 50 microns

Cat. No. SNW-01-1
Specification 80 nm
Unit Size 1 mL
Price $385.00

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Silver Nanowire, conductive, diameter 80 nm, length, 50 microns Cat. No. SNW-01-2 80 nm 5 mL修饰性聚乙二醇

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上海金畔生物科技有限公司提供各种分子量和基团修饰性聚乙二醇定制服务。

Silver Nanowire, conductive, diameter 80 nm, length, 50 microns

Cat. No. SNW-01-2
Specification 80 nm
Unit Size 5 mL
Price $885.00

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Thienopyridone

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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。

Thienopyridone  纯度: 98.04%

Thienopyridone 是一种有效的选择性的肝再生磷酸酶 (PRL) 磷酸酶抑制剂，对于 PRL-1，PRL-2 和 PRL-3，IC50 值分别为 173 nM，277 nM 和 128 nM。Thienopyridone 对其他磷酸酶的影响很小。Thienopyridone 可诱导 p130Cas 裂解和细胞凋亡 (apoptosis)，并具有抗癌作用。

Thienopyridone

Thienopyridone Chemical Structure

CAS No. : 1018454-97-1

规格 价格 是否有货 数量
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Thienopyridone 相关产品

•相关化合物库:

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

生物活性

Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1].

IC50 & Target

IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)[1]
体外研究
(In Vitro)

Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC50 values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively[1].
Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. Thienopyridone induces the cleavage of PARP and caspase-8[1].
Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation[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: RKO and HT-29 cells
Concentration: 0.5 μM, 1.67 μM, 5 μM, 8.33 μM
Incubation Time: 14 days
Result: Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM
Incubation Time: 24 hours
Result: A dose-dependent down-regulation of total p130Cas was observed.

分子量

242.30

Formula

C13H10N2OS
CAS 号

1018454-97-1
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 : 5 mg/mL (20.64 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1271 mL 20.6356 mL 41.2712 mL
5 mM 0.8254 mL 4.1271 mL 8.2542 mL
10 mM 0.4127 mL 2.0636 mL 4.1271 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 (8.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.58 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]. Daouti S, et al. A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage. Cancer Res. 2008 Feb 15;68(4):1162-9.

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

MASTER-SUR/NM|MASTER-SUR/Nα临床折射仪

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【简单介绍】

MASTER-SUR/NM|MASTER-SUR/Nα临床折射仪 它在材料上采用的树脂具有耐盐性及耐酸性，可以防止腐蚀。这款带防水功能及自动温度补偿功能。

【详细说明】

MASTER-SUR/NM|MASTER-SUR/Nα临床折射仪

MASTER-SUR/NM临床折射仪

MASTER-SUR/NM是临床用折射仪，它是测量血清蛋白，尿比重以及折射率的产品。它在材料上采用的树脂具有耐盐性及耐酸性，可以防止腐蚀。与MASTER-SUR/NM不同，这款没有带防水功能及自动温度补偿功能。您可以手动校正。
型号
MASTER-SUR/NM
货号
2773
標度範圍
尿比重标度 : 1.000 至 1.060
血清蛋白质标度 : 0.0 至 12.0g/10 0毫升
屈折指数标度 : nD 1.3330 至 1.3660
小標度
尿比重标度: 0.001
血清蛋白质标度 : 0.2公克/100毫升
折射指数标度 : （nD） 0.0005
選件
• MASTER 系列 微量样品用棱镜盖 : RE-2391-50M （粘度高的产品除外）
消耗品/零件
MASTER 系列 日光板 : RE-2391-59M
尺寸重量
3.2×3.4×20.3公分,
105公克
 
 
MASTER-SUR/Nα临床折射仪（自动温度补偿&防水）
MASTER-SUR/Nα是临床用折射仪，它是测量血清蛋白，尿比重以及折射率的产品。它在材料上采用的树脂具有耐盐性及耐酸性，可以防止腐蚀。这款带防水功能及自动温度补偿功能。
型号
MASTER-SUR/Nα
货号
2771
標度範圍
（ 自動溫度補償功能 ）
尿比重标度 : 1.000 至 1.060
血清蛋白质标度 : 0.0 至 12.0g/100 毫升
屈折指数标度 : nD 1.3330 至 1.3660
小標度
尿比重标度: 0.001
血清蛋白质标度 : 0.2公克/100毫升
折射指数标度 : （nD） 0.0005
測量準確度
（10 至 30°C ）
尿比重标度 : ±0.001
血清蛋白质标度 : ±0.2公克/100 毫升
折射指数标度 : （nD） ±0.0005
國際保護等級
IP65 （接眼部以外的部分）
無塵且對噴射水柱具防護作用
尺寸重量
3.2×3.4×20.3公分,
105公克
選件
• MASTER 系列 微量样品用棱镜盖 : RE-2391-50M （粘度高的产品除外）
消耗品/零件
MASTER 系列 日光板 : RE-2391-59M
 
上海金畔生物科技有限公司：
：
 
：崔
：azlqxb@.cn
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UV-6100S大屏幕扫描型紫外可见分光光度计

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【简单介绍】

UV-6100S大屏幕扫描型紫外可见分光光度计采用悬架式光学系统设计，整体光路独立固定在16mm厚的切削铝制无变形基座上，底板的变形和外界的震动对光学系统不产生任何影响，从而大大提高了仪器的稳定性和可靠性。

【详细说明】

UV-6100S大屏幕扫描型紫外可见分光光度计

 

仪器指标

波长范围

190-1100nm

光谱带宽

 0.5/1.0/2.0/4.0/5.0nm（可调）

波长准确度

 ±0.1nm@656.1nm,±0.3nm全区域

波长重复性

 ≤0.1nm

光度准确度

±0.2%T（0-T）

±0.002Abs(0-0.5Abs)

±0.004Abs(0.5-1Abs)

光度重复性

 ≤0.1%T(0-T)

0.001Abs(0-0.5Abs)

0.002Abs(0.5-1Abs)

杂散光

≤0.03%T@220nm,360nm

稳定性

 ±0.0005A/h（500nm处）

基线平直度

 ±0.001A

噪声水平

 ±0.0004A

光度范围

0-200%T

-4.0-4.0A

0-9999C

数据输出

USB接口

打印输出

 并行口

显示系统

320*240位大屏幕LCD

光源

 进口长寿命钨灯、氘灯

检测器

 进口硅光二极管

外形尺寸

625*430*210mm

电源

AC 220V/50Hz或110V/60Hz

重量

28kg

UV-6100S大屏幕扫描型紫外可见分光光度计

特点功能：

◆UV-6100S型可实现0.5/1.0/2.0/4.0/5.0nm五档光谱带宽自动可调

◆采用320*240位点阵式高亮6 ”液晶显示器，显示清晰，信息完备
◆强大的数据分析功能，主机可独立完成光度测量、定量测量、光谱扫描、动力学、DNA/蛋白质测试，多波长测试及数据打印等功能

◆采用悬架式光学系统设计，整体光路独立固定在16mm厚的切削铝制无变形基座上，底板的变形和外界的震动对光学系统不产生任何影响，从而大大提高了仪器的稳定性和可靠性
◆主要元件采用进口配置，使仪器杂散光更低、稳定性、可靠性更强

◆充分考虑不同用户的使用习惯，本系列仪器都标配元析公司光谱扫描软件，联机操作时，除能实现主机的所有测试功能外，还可实现更为强大的数据处理功能，并且使数据存储达到无限

AZD4320

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。

AZD4320  纯度: 99.10%

AZD4320 是 BH-3 的新型类似物，有效的 BCL2/BCLxL 的双重抑制剂。AZD4320 对于 KPUM-MS3，KPUM-UH1，和 STR-428 细胞系的 IC50 分别为 26 nM，17 nM，和 170 nM。

AZD4320

AZD4320 Chemical Structure

CAS No. : 1357576-48-7

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2550 In-stock
5 mg ￥1750 In-stock
10 mg ￥2450 In-stock
50 mg ￥8250 In-stock
100 mg ￥14500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AZD4320 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library
  • Anti-Blood Cancer Compound Library

生物活性

AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.

IC50 & Target

BCL2

17 nM (IC50, KPUM-UH1 cells)

BCLxL

17 nM (IC50, KPUM-UH1 cells)

体外研究
(In Vitro)

AZD4320 potently augments the antitumor effect of AZD5153 (Cat. No.: HY-100653A) in double expressing lymphoma (DEL)- and double hit lymphoma (DHL)-derived cell lines in a dose-dependent manner. AZD4320 shows mostly synergistic, and at least additive, growth inhibitory effects on DEL- and DHL derived cell lines, and profoundly increases cells undergoing apoptosis in all three cell lines[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

945.53

Formula

C45H48ClF3N4O7S3
CAS 号

1357576-48-7
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 : 125 mg/mL (132.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0576 mL 5.2880 mL 10.5761 mL
5 mM 0.2115 mL 1.0576 mL 2.1152 mL
10 mM 0.1058 mL 0.5288 mL 1.0576 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: ≥ 6.25 mg/mL (6.61 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (6.61 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 62.5 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

*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]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.
Cell Assay
[1]

Two DEL-derived cell lines, KPUM-MS3 and KPUM-UH1, and a DHL-derived cell line, STR-428 are used. To examine the combinatory growth inhibitory effects of AZD4320, cells are treated with five concentrations (0.25, 0.5, 1.0, 2.0, 4.0×IC50) for 72 h, and subjected to a modified MTT 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.
参考文献

  • [1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.

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

NDI-091143

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。

NDI-091143  纯度: 99.94%

NDI-091143 是一种有效的高亲和力人 ATP 柠檬酸裂解酶 (ACLY) 抑制剂，IC50 为 2.1 nM (ADP-Glo分析)，Ki 为 7.0 nM，Kd 为 2.2 nM。NDI-091143 通过稳定柠檬酸盐域中的大构象变化来间接抑制柠檬酸的结合和识别，从而抑制了 ACLY 催化变构反应。

NDI-091143

NDI-091143 Chemical Structure

CAS No. : 2375840-87-0

规格 价格 是否有货 数量
5 mg ￥875 In-stock
10 mg ￥1500 In-stock
25 mg ￥3125 In-stock
50 mg ￥5625 In-stock
100 mg ￥9375 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NDI-091143 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Lipid Metabolism Compound Library

生物活性

NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate[1].

IC50 & Target

IC50: 2.1 nM (human ATP-citrate lyase); Ki: 7.0 nM (human ATP-citrate lyase); Kd: 2.2 nM (human ATP-citrate lyase)[1]
体外研究
(In Vitro)

Thermal shift assays shows that NDI-091143 gives rise to considerable stabilization of both full-length ACLY and the N-terminal segment. The thermal shift data are consistent with limited proteolysis experiments using full-length ACLY, in which NDI-091143 together with Mg-ATP provided the greatest protection against digestion by chymotrypsin[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

453.84

Formula

C20H14ClF2NO5S
CAS 号

2375840-87-0
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 (220.34 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 2.2034 mL 11.0171 mL 22.0342 mL
5 mM 0.4407 mL 2.2034 mL 4.4068 mL
10 mM 0.2203 mL 1.1017 mL 2.2034 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 (4.58 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
  • 3.

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

    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，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]. Wei J, et al. An allosteric mechanism for potent inhibition of human ATP-citrate lyase. Nature. 2019 Apr;568(7753):566-570.

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

CPL304110

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。

CPL304110  纯度: 99.68%

CPL304110 是有效的、口服有效的、选择性的成纤维细胞生长因子受体 FGFR (1-3) 的抑制剂，其对 FGFR (1-3) 的 IC50 值分别为 0.75 nM、0.5 nM 和 3.05 nM。

CPL304110

CPL304110 Chemical Structure

CAS No. : 1627826-19-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥2500 In-stock
10 mg ￥4000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CPL304110 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively[1].

IC50 & Target[1]

FGFR1

0.75 nM (IC50)

FGFR2

0.5 nM (IC50)

FGFR3

3.05 nM (IC50)

体外研究
(In Vitro)

CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK)[1].
CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC50 of 85.64 nM[1].
CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases[1].

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

Western Blot Analysis[1]

Cell Line: SNU-16 cell lines.
Concentration: 0-0.6 μM.
Incubation Time: 1 h.
Result: Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK)

体内研究
(In Vivo)

CPL304110 (p.o., 40 mg/kg) exhibits a t1/2 of 2 h and Cmax of 3369 ng/mL in mice[1].
CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day[1].

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

Animal Model: Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human)[1].
Dosage: 20 mg/kg (X2).
Administration: Orally, twice daily for 21 days.
Result: After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%).

Clinical Trial

分子量

446.54

Formula

C25H30N6O2
CAS 号

1627826-19-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (223.94 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2394 mL 11.1972 mL 22.3944 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Abdellah Yamani, et al. Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). Eur J Med Chem. 2020 Nov 7;112990.

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

GSK778(Synonyms: iBET-BD1)

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。

GSK778 (Synonyms: iBET-BD1) 纯度: 99.25%

GSK778 (iBET-BD1) 是一种有效和选择性的 BET 蛋白 BD1 溴结构域的抑制剂，IC50 值为 75 nM (BRD2 BD1)，41 nM (BRD3 BD1)，41 nM (BRD4 BD1) 和143 nM (BRDT BD1)。GSK778 表型化了 pan-BET 抑制剂在癌症模型中的作用。

GSK778(Synonyms: iBET-BD1)

GSK778 Chemical Structure

CAS No. : 2451862-42-1

规格 价格 是否有货 数量
5 mg ￥7000 In-stock
10 mg ￥12000 In-stock
25 mg ￥25000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GSK778 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1].

IC50 & Target[1]

BRD2 BD1

75 nM (IC50)

BRD3 BD1

41 nM (IC50)

BRD4 BD1

41 nM (IC50)

BRDT BD1

143 nM (IC50)

体外研究
(In Vitro)

GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively[1].
GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22[1].
GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells[1].
GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells[1].
GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML 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.

Cell Proliferation Assay[1]

Cell Line: Human primary CD4+ T cell
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited the proliferative activity of the cells and the production of effector cytokines.

Cell Viability Assay[1]

Cell Line: MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited the growth and viability of human cancer cell lines.

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM13, MDA-MB-231 and MB453 cells
Concentration: 1000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.

体内研究
(In Vivo)

GSK778 (15 mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model[1].
GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1].
GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10 mg/kg) in 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.

Animal Model: 6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells[1]
Dosage: 15 mg/kg/BID
Administration: I.p. injections for 30 days
Result: Increased the survival rate of leukemia mice.
Animal Model: Male CD1 mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: P.o. administration
Result: Cmax (85 ng/mL), Tmax (1.48 h); AUC∞ (132 ng.h/mL).

分子量

511.61

Formula

C30H33N5O3
CAS 号

2451862-42-1
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 : 41.67 mg/mL (81.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9546 mL 9.7731 mL 19.5461 mL
5 mM 0.3909 mL 1.9546 mL 3.9092 mL
10 mM 0.1955 mL 0.9773 mL 1.9546 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 (4.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.07 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 (4.07 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.07 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 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 (4.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.07 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 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]. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394.

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

Nampt-IN-5

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。

Nampt-IN-5  纯度: 99.21%

Nampt-IN-5 是一种有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 抑制剂。Nampt-IN-5 还抑制 CYP3A4 活性。Nampt-IN-5 可抑制 A2780 和 COR-L23 细胞，IC50 值分别为 0.7 nM 和 3.9 nM。

Nampt-IN-5

Nampt-IN-5 Chemical Structure

CAS No. : 2380013-17-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4400 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.

Nampt-IN-5 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library

生物活性

Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1].

IC50 & Target

NAMPT[1]
CYP3A4[1]
体外研究
(In Vitro)

Nampt-IN-5 (compound 27) (0-10 nM; 3 days) has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively [1].
Nampt-IN-5 shows a good ADME data: mouse microsomal clearance (110 μl/min•mg), CYP3A4 inhibition value (0.75 μM), Sol6.8: 0.056 mM; MDCK Papp AB: 18.6[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Nampt-IN-5 (5-30 mg/kg; p.o. twice daily for 4 days) causes a significant amount of body weight loss in nude mice relative to vehicle[1].
Nampt-IN-5 (10 mg/kg; p.o.) exhibits T1/2 (2.1 h), Cmax (29112 nM), and AUC (61984 nM•h) in mice[1].

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

427.50

Formula

C25H25N5O2
CAS 号

2380013-17-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (116.96 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 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 (5.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.85 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% corn oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.85 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Palacios DS, et al. Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529.

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

BET bromodomain inhibitor 1

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。

BET bromodomain inhibitor 1  纯度: 99.91%

BET bromodomain inhibitor 1 是一种具有口服活性的，选择性 BET 溴结构域抑制剂，对 BRD4 的 IC50 为 2.6 nM。BET bromodomain inhibitor 1 与 BRD2(2)，BRD3(2)，BRD4(1)，BRD4(2) 和 BRDT(2) 高亲和力结合 (Kd 值分别为 1.3 nM、1.0 nM、3.0 nM、1.6 nM、2.1 nM)。BET bromodomain inhibitor 1 具有抗癌活性。

BET bromodomain inhibitor 1

BET bromodomain inhibitor 1 Chemical Structure

CAS No. : 2411226-02-1

规格 价格 是否有货 数量
5 mg ￥3800 In-stock
10 mg ￥6000 In-stock
25 mg ￥11500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

BET bromodomain inhibitor 1 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
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity[1].

IC50 & Target[1]

BRD4

2.6 nM (IC50)

BRD2(2)

1.3 nM (Kd)

BRD3(2)

1.0 nM (Kd)

BRD4(1)

3.0 nM (Kd)

BRD4(2)

1.6 nM (Kd)

BRDT(2)

2.1 nM (Kd)

体外研究
(In Vitro)

BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest[1].
BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels[1].
BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6[1].
BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC50>20 μM)[1].
BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ∼1500-fold selectivity for BRD4(1) over EP300 (IC50=3857 nM)[1].
BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively[1].

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

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125 nM
Incubation Time: 24 hours
Result: Led to more pronounced G1-phase cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125, 250, 500 nM
Incubation Time: 6 or 24 hours
Result: Induced dose-dependent inhibition on c-Myc expression and upregulation of p21 levels.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125 nM
Incubation Time: 6 hours
Result: Robustly reduced the expressions of c-Myc, BCL-2, and CDK6.

体内研究
(In Vivo)

BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg[1].
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min•kg, and a Vss of 1464 and 782 mL/kg for rats and mouse, respectively[1].
BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T1/2 of 3.6 hours, a Cmax of 159 ng/mL and an AUC of 884 ng•h/mL for rats[1].
BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T1/2 of 1.3 hours, a Cmax of 399 ng/mL and an AUC of 1710 ng•h/mL for mouse[1].

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

Animal Model: An MV4-11 mouse xenograft model[1]
Dosage: 6.25, 12.5 mg/kg
Administration: PO; daily ; for 28 days
Result: Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
Animal Model: Male SD rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a Vss of 1464 mL/kg.

分子量

459.47

Formula

C22H19F2N3O4S
CAS 号

2411226-02-1
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 : 62.5 mg/mL (136.03 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 2.1764 mL 10.8821 mL 21.7642 mL
5 mM 0.4353 mL 2.1764 mL 4.3528 mL
10 mM 0.2176 mL 1.0882 mL 2.1764 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: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.44 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。

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.53 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.53 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Zizhou Li, et al. Discovery of 8-Methyl-pyrrolo[1,2- a]pyrazin-1(2 H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors. J Med Chem. 2020 Apr 23;63(8):3956-3975.

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

Olafertinib

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。

Olafertinib  纯度: 99.41%

Olafertinib 是三代 EGFR 酪氨酸酶抑制剂，其GI50 值分别为5 nM (EGFR L858R/T790M)、10 nM (EGFR del19) 和 689 nM (EGFR WT)。

Olafertinib

Olafertinib Chemical Structure

CAS No. : 1660963-42-7

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 ￥2568 In-stock
5 mg ￥2200 In-stock
10 mg ￥3500 In-stock
25 mg ￥6500 In-stock
50 mg ￥9000 In-stock
100 mg ￥14000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Olafertinib 相关产品

•相关化合物库:

  • Covalent Screening 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
  • Covalent Screening 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

Olafertinib is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. Olafertinib has the potential for NSCLC research[1].

IC50 & Target

GI50: 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19), 689 nM (EGFR WT)[1].
分子量

530.57

Formula

C29H28F2N6O2
CAS 号

1660963-42-7
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 : 125 mg/mL (235.60 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8848 mL 9.4238 mL 18.8477 mL
5 mM 0.3770 mL 1.8848 mL 3.7695 mL
10 mM 0.1885 mL 0.9424 mL 1.8848 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 (3.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.92 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 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: ≥ 2.08 mg/mL (3.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.92 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]. Misako Nagasaka, et al. Beyond osimertinib: The development of 3 rd-generation EGFR Tyrosine Kinase Inhibitors. J Thorac Oncol. 2020 Dec 15;S1556-0864(20)31105-9.

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

JAK2/FLT3-IN-1

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。

JAK2/FLT3-IN-1 

JAK2/FLT3-IN-1 是一种口服有效的双重 JAK2/FLT3 抑制剂，对 JAK2，FLT3，JAK1 和 JAK3 的 IC50 分别为 0.7 nM，4 nM，26 nM 和 39 nM。JAK2/FLT3-IN-1 具有抗癌活性。

JAK2/FLT3-IN-1

JAK2/FLT3-IN-1 Chemical Structure

CAS No. : 2387765-27-5

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

* Please select Quantity before adding items.

JAK2/FLT3-IN-1 的其他形式现货产品:

JAK2/FLT3-IN-1 TFA

生物活性

JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity[1].

IC50 & Target[1]

JAK2

0.7 nM (IC50)

FLT3

4 nM (IC50)

JAK1

26 nM (IC50)

JAK3

39 nM (IC50)

体外研究
(In Vitro)

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].

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

Western Blot Analysis[1]

Cell Line: MV4-11 and SET-2 cells
Concentration: 0.008, 0.04, 0.2, 1 μM
Incubation Time: For 2 hours
Result: Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.

体内研究
(In Vivo)

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects[1].

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

Animal Model: NOD/SCID mouse models[1]
Dosage: 30 and 60 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

分子量

467.58

Formula

C25H34FN7O
CAS 号

2387765-27-5
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.
溶解性数据
In Vitro: 

DMSO : 20.83 mg/mL (44.55 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 2.1387 mL 10.6934 mL 21.3867 mL
5 mM 0.4277 mL 2.1387 mL 4.2773 mL
10 mM 0.2139 mL 1.0693 mL 2.1387 mL

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 (4.45 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.45 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 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 (4.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.45 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 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

E7090 succinate

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。

E7090 succinate 

E7090 succinate 是具有口服活性的、选择性的、有效的 FGFR1/2/3 抑制剂，其对 FGFR1/2/3/4 的 IC50 值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。

E7090 succinate

E7090 succinate Chemical Structure

CAS No. : 1879965-80-6

规格 价格 是否有货
5 mg ￥8500 询问价格 & 货期
10 mg ￥14500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].

IC50 & Target[2]

FGFR1

0.71 nM (IC50)

FGFR2

0.50 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

120 nM (IC50)

体外研究
(In Vitro)

E7090 also inhibited the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM[1].
E7090 succinate inhibited SNU-16 cell proliferation with an IC50 value of 5.7 nM[2].
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling[1].
E7090 succinate has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes[1].

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

Western Blot Analysis[1]

Cell Line: SNU-16 cells.
Concentration: 0.4-100 nM.
Incubation Time: 4 h.
Result: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nmol/L. Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.

体内研究
(In Vivo)

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner. Overall, the in vitro and in vivo studies confirm that E7090 is a potent and selective FGFRs inhibitor, showing promising antitumor activities with wider therapeutic windows in preclinical cancer models harboring FGFRs gene abnormalities[1]. E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2.

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

Animal Model: Mouse xenograft model of SNU-16 human gastric cancer[2].
Dosage: 6.25 to 50 mg/kg.
Administration: Orally, once daily for 14 days.
Result: Inhibited tumor growth in a dose-dependent manner.

Clinical Trial

分子量

764.82

Formula

C36H43N5O10
CAS 号

1879965-80-6
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]. Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

    [2]. Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15(11):2630-2639.

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

JX06

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。

JX06  纯度: 99.88%

JX06 是一种有效的，选择性的，共价的 PDK 抑制剂。JX06 抑制 PDK1, PDK2 和 PDK3，IC50 值分别为 49 nM，101 nM 和 313 nM。JX06 以不可逆的方式与半胱氨酸残基共价结合来抑制 PDK1 活性。JX06 具有抗肿瘤活性。

JX06

JX06 Chemical Structure

CAS No. : 729-46-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥800 In-stock
25 mg ￥1800 In-stock
50 mg ￥3000 In-stock
100 mg ￥5000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JX06 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Glycolysis Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity[1].

IC50 & Target

IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)[1]
体外研究
(In Vitro)

JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM[1].
JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR[1].
JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells[1].
JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner[1].
JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells[1].
JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) [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.

Apoptosis Analysis[1]

Cell Line: A549, EBC-1, HT-29 and H460 cells
Concentration: 0, 1, 3, 10 μM
Incubation Time: 48 hours
Result: Induces cell apoptosis in A549 and EBC-1 cells.

Cell Viability Assay[1]

Cell Line: A549 cells
Concentration: 0, 0.2, 0.4, 0.6 μM
Incubation Time: 72 hours
Result: Inhibits the viability of A549 cells in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 0, 6, 12, 24 hours
Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.

体内研究
(In Vivo)

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo[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: A549 subcutaneous xenograft mice[1]
Dosage: 40, 80 mg/kg
Administration: I.p. injections for 21 days
Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.
Well tolerated at the administration dose.

分子量

324.51

Formula

C10H16N2O2S4
CAS 号

729-46-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (154.08 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0816 mL 15.4078 mL 30.8157 mL
5 mM 0.6163 mL 3.0816 mL 6.1631 mL
10 mM 0.3082 mL 1.5408 mL 3.0816 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 (7.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.70 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 (7.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.70 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 (7.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.70 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]. Wenyi S, et, al. JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. Cancer Res. 2015 Nov 15; 75(22): 4923-36.

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

E7090

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。

E7090 

E7090 是一种有效的，具有口服活性的选择性 FGFR 抑制剂，对 FGFR1/FGFR2/FGFR3/FGFR4 的 IC50 值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。

E7090

E7090 Chemical Structure

CAS No. : 1622204-21-0

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

E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively[1].

IC50 & Target[2]

FGFR1

0.71 nM (IC50)

FGFR2

0.50 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

120 nM (IC50)

体外研究
(In Vitro)

E7090 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM[1].
E7090 inhibits SNU-16 cell proliferation with an IC50 value of 5.7 nM[2].
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling[1].
E7090 has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes[1].

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

Western Blot Analysis[1]

Cell Line: SNU-16 cells
Concentration: 0.4-100 nM
Incubation Time: 4 hours
Result: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nM.
Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.

体内研究
(In Vivo)

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2].

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

Animal Model: Mouse xenograft model of SNU-16 human gastric cancer[2]
Dosage: 6.25 to 50 mg/kg
Administration: Orally, once daily for 14 days
Result: Inhibited tumor growth in a dose-dependent manner.

Clinical Trial

分子量

587.67

Formula

C32H37N5O6
CAS 号

1622204-21-0
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]. Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

    [2]. Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15(11):2630-2639.

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UNC2025

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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。

UNC2025  纯度: 99.94%

UNC2025 是一种强效、ATP 竞争性的，具有口服活性的 Mer/Flt3 抑制剂，IC50 值分别为 0.74 nM 和 0.8 nM。UNC2025 对MERTK 的选择性是 Axl 的 45 倍 (IC50=122 nM; Ki=13.3 nM)。UNC2025 具有良好的 PK 特性，可用于急性白血病的研究。

UNC2025

UNC2025 Chemical Structure

CAS No. : 1429881-91-3

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1049 In-stock
2 mg ￥600 In-stock
5 mg ￥1000 In-stock
10 mg ￥1700 In-stock
25 mg ￥2800 In-stock
50 mg ￥4800 In-stock
100 mg ￥8000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia[1].

IC50 & Target

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)[1]
体外研究
(In Vitro)

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively[1].
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50 of 2.7 nM in 697 B-ALL cells[1].
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells[1].
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells[1].
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells[2].
UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2[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[1]

Cell Line: 32D Cells
Concentration: 0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
Incubation Time: 1 hour
Result: Inhibited p-MEK, p-AXL, p-TYRO3 expression

Cell Viability Assay[2]

Cell Line: Mononuclear cells 
Concentration: 14 nM–10μM
Incubation Time: 48 hour
Result: Showed IC50 values ranged from 9.0 nM to >10μ M with a median IC50 of 2.38 μM.

Western Blot Analysis[2]

Cell Line: MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines
Concentration: 25-300 nM
Incubation Time: 1 hour
Result: Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.

体内研究
(In Vivo)

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively[2].
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, 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.

Animal Model: NSG mice injected with 697 B-ALL cells[2]
Dosage: 50 or 75 mg/kg
Administration: Orally adminstration
Result: Delayed the disease progression.

分子量

476.66

Formula

C28H40N6O
CAS 号

1429881-91-3
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 (69.92 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0979 mL 10.4897 mL 20.9793 mL
5 mM 0.4196 mL 2.0979 mL 4.1959 mL
10 mM 0.2098 mL 1.0490 mL 2.0979 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 (5.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.24 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% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.24 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]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41.

    [2]. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

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Copanlisib dihydrochloride(Synonyms: 库潘尼西盐酸; BAY 80-6946 dihydrochloride)

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。

Copanlisib dihydrochloride (Synonyms: 库潘尼西盐酸; BAY 80-6946 dihydrochloride) 纯度: 99.55%

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 是一种有效的，选择性的和 ATP 竞争性的泛 I 类 PI3K 抑制剂，对 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ 的 IC50 分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除 mTOR 外，Copanlisib dihydrochloride 对其他脂质和蛋白激酶的选择性超过 2000 倍。Copanlisib dihydrochloride 具有优异的抗肿瘤活性。

Copanlisib dihydrochloride(Synonyms: 库潘尼西盐酸; BAY 80-6946 dihydrochloride)

Copanlisib dihydrochloride Chemical Structure

CAS No. : 1402152-13-9

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生物活性

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity[1].

IC50 & Target[1]

PI3Kα

0.5 nM (IC50)

PI3Kδ

0.7 nM (IC50)

PI3Kβ

3.7 nM (IC50)

PI3Kγ

6.4 nM (IC50)

mTOP

45 nM (IC50)

体外研究
(In Vitro)

Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1].
Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells[1].
Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[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.

Apoptosis Analysis[1]

Cell Line: BT20 breast cancer cells
Concentration: 20 nM and 62 nM, 200 nM
Incubation Time: 24 hours
Result: Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC50 of 340 nM.

Western Blot Analysis[1]

Cell Line: ELT3 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 500 nM
Incubation Time: 2 hours
Result: Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.

体内研究
(In Vivo)

Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model[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: Athymic nude rats injected with KPL4 tumor cells[1]
Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg
Administration: Intravenous injection; every second day, every third day; for 60 days
Result: On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.

Clinical Trial

分子量

553.44

Formula

C23H30Cl2N8O4
CAS 号

1402152-13-9
中文名称

库潘尼西盐酸
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 : 20 mg/mL (36.14 mM; Need ultrasonic)

DMSO : 5 mg/mL (9.03 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 1.8069 mL 9.0344 mL 18.0688 mL
5 mM 0.3614 mL 1.8069 mL 3.6138 mL
10 mM 0.1807 mL 0.9034 mL 1.8069 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]. Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30.

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RET-IN-4

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。

RET-IN-4 

RET-IN-4 是一种有效、选择性和具有口服活性的 RET 抑制剂，对 RET (WT)，RET (V804M) 和 RET (M918T) 的 IC50 分别为 1.29 nM，1.97 nM 和 0.99 nM。RET-IN-4 对 JAK2 (IC50 为 4.4 nM) 和 FLT3 (IC50 为 30.8 nM) 表现出更好的激酶选择性。RET-IN-4 具有抗癌作用。

RET-IN-4

RET-IN-4 Chemical Structure

CAS No. : 2436473-55-9

规格 是否有货
100 mg   询价  
250 mg   询价  
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生物活性

RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects[1].

IC50 & Target

IC50: 1.29 nM (RET (WT)), 1.97 nM (RET (V804M)), and 0.99 nM (RET (M918T))[1]
体外研究
(In Vitro)

The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner[1].

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

Animal Model: Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: p.o.; daily; for 10 days
Result: The tumor growth was remarkably suppressed.

分子量

546.60

Formula

C27H31FN10O2
CAS 号

2436473-55-9
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]. Zhibo Luo, et al. Discovery and Optimization of Selective RET Inhibitors via Scaffold Hopping. Bioorg Med Chem Lett. 2021 May 28;128149.

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