Defactinib 是新型的 FAK 抑制剂，能够时间和剂量依赖性的抑制 FAK 在 Tyr397 位点磷酸化。

Defactinib is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

在PTX敏感和PTX耐药模型中,口服VS-6063（50 mg/kg）,能够产生生长抑制作用.

在紫杉醇敏感的(SKOV3ip1)和紫杉醇耐药的(SKOV3-TR)细胞系中,VS-6063抑制pFAK (Tyr397)表达。在甲状腺癌细胞系中,VS-6063 和Y15协调作用能够抑制细胞黏附和增殖。在SKOV3ip1,SKOV3-TR,HeyA8 和HeyA8-MDR细胞中,VS-6063和紫杉醇协同降低细胞增殖,诱导细胞凋亡。

Cell-free Kinase Activity Assays: IC50 values for TG101348 are determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration is set to approximately the Km value for each kinase.

Ovarian cancer cells are treated with increasing concentrations of VS-6063 for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments.(Only for Reference)

1073154-85-4

C20H21F3N8O3S

510.49

VS-6063;PF-04554878

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years