SAR-020106
| CAS号 | 1184843-57-9 | 货号 | BCP29578 |
| 中文名 | SAR-020106 | ||
| 英文名 | SAR-020106 | ||
| 中文别名 | |||
| 英文别名 | SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106; | ||
| 分子式 | C19H19ClN6O | 分子量 | 382.85 |
| 生物活性 | 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. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | Checkpoint | ||
结构式
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