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发布者：信康 浏览次数：
产品名称:N/ACAS:1073154-85-4别名：VS-6063;PF-04554878英文名：Defactinib
[] - 生物活性Defactinib (VS-6063, PF-04554878)是一种选择性，且口服有效的FAK抑制剂。Phase 2。
- 体外研究In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines.
- 体内研究In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
