CHIR-124

产品说明书

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Chemical Structure| 405168-58-3 同义名 : -
CAS号 : 405168-58-3
货号 : A241808
分子式 : C23H22ClN5O
纯度 : 98%
分子量 : 419.91
MDL号 : MFCD14636453
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 6 mg/mL(14.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Chk1

    Chk1, IC50:0.3 nM
描述 CHIR-124 is a potent Chk1 inhibitor with IC50 of 0.3 nM with 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human MDA-MB-435 cells Cytotoxic assay Cytotoxicity against human MDA-MB-435 cells, EC50=0.08 μM 16603354
human MDA-MB-435 cells Cytotoxic assay Cytotoxicity against human MDA-MB-435 cells in presence of camptothecin 16603354
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.81mL

4.76mL

2.38mL
参考文献

[1]Dai Y, Grant S. New insights into checkpoint kinase 1 in the DNA damage response signaling network. Clin Cancer Res. 2010 Jan 15;16(2):376-83.

[2]Tse AN, Rendahl KG, et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602.