Defactinib(PF-04554878)CAS号： 1073154-85-4分子式： C20H21F3N8O3S分子量： 510.49描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
Defactinib (VS-6063, PF-04554878)是一种选择性，有效的FAK抑制剂。 |
| 纯度 |
98% min
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
VS-6063; VS6063; VS 6063; PF04554878; PF-04554878; PF 04554878
|
| 可溶性/溶解性 |
DMSO 5 mg/mL warmed (9.79 mM)
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| 生物活性 | |
| 靶点 |
FAK
|
| In vitro(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.
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| In vivo(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.
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分子结构图
