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CAS No.: 1184843-57-9
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.
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实验方案
技术信息
CAS号 | 1184843-57-9 | 储存条件 |
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分子式 | C19H19ClN6O | 运输 | 蓝冰 | |
分子量 | 382.85 | 别名 |
Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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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 |
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