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SAR-020106

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Chemical Structure| 1184843-57-9 同义名 : -
CAS号 : 1184843-57-9
货号 : A547402
分子式 : C19H19ClN6O
纯度 : 98%
分子量 : 382.847
MDL号 : MFCD28155090
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(10.45 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
动物实验配方：
生物活性
靶点

  • Chk1

    Chk1, IC50:13.3 nM
描述 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC (50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G (2) arrest with an IC (50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK cells Function assay Inhibition of human ERG overexpressed in HEK cells, IC50=5 μM 23082860
HT-29 cells Function assay Antimitotic activity in etoposide-induced human HT-29 cells assessed as induction of M-phase phosphoprotein 2 expression by ELISA, IC50=0.055 μM 22111927
SW620 cells Function assay Inhibition of CHK1 in human SW620 cells assessed as potentiation of gemcitabine-induced cytotoxicity after 24 to 48 hrs 23082860
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.06mL

2.61mL

1.31mL

26.12mL

5.22mL

2.61mL
参考文献

[1]Reader JC, Matthews TP, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011 Dec 22;54(24):8328-42.

[2]Walton MI, Eve PD, et al. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010 Jan;9(1):89-100.