地法替尼盐酸盐
| CAS号 | 1073160-26-5 | 货号 | BCP17737 |
| 中文名 | 地法替尼盐酸盐 | ||
| 英文名 | Defactinib hydrochloride | ||
| 中文别名 | |||
| 英文别名 | PF-04554878 hydrochloride;PF04554878 hydrochloride;PF 04554878 hydrochloride;VS6063 hydrochloride;VS 6063 hydrochloride;VS6063 hydrochloride; | ||
| 分子式 | C20H22ClF3N8O3S | 分子量 | 546.95 |
| 生物活性 | VS-6063 inhibited FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. The combination of VS-6063 and paclitaxel markedly decreased proliferation and increased apoptosis, which resulted in 92.7% to 97.9% reductions in tumor weight. RPPA data showed that VS-6063 reduced levels of AKT and YB-1 in taxane-resistant cell lines. FAK inhibition enhanced chemosensitivity in taxane-resistant cells by decreasing YB-1 phosphorylation and subsequently CD44 in an AKT-dependent manner. | ||
| 上下游产品 | 1073154-85-4（地法替尼） 1345713-71-4（地法替尼） | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase PI3K/Akt/mTOR | ||
| 靶 点 | PI3K FAK | ||
结构式
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