FAK-IN-2 是一种有效且具有口服活性的黏着斑激酶 (FAK) 抑制剂，具有抗肿瘤活性 (FAKIC50= 35 nM)。FAK-IN-2 以剂量依赖的方式共价抑制 FAK 的自磷酸化，也能抑制肿瘤细胞的形成和迁移，诱导其凋亡。

FAK-IN-2 is a potent and orally active focal adhesion kinase ( FAK ) inhibitor, with anticancer activity (FAK IC 50 = 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis [1].

FAK-IN-2 (compound 11w) (0-5 μM; 72 hours) has high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines [1]. FAK-IN-2 (0-30 nM; 14 days) can remarkably affect HCT-116 cells clone formation in a dose-dependent manner [1]. FAK-IN-2 (10-500 nM; 24 and 48 hours) significantly inhibits the migration of HCT116 cells at both 24 h and 48 h in a dose-dependent manner [1]. FAK-IN-2 (0.001-10 μM; 4 and 24 hours) inhibits the phosphorylation of FAK and its downstream proteins from multiple pathways [1]. FAK-IN-2 (0.01-1 μM; 24 or 48 hours) induces strong cell cycle arrest at the G2/M phase and apoptosis [1]. Cell Proliferation Assay Cell Line: Hela, HCT116, MDA-MB-231, H9C2, L929, LO2, HEK293 [1] Concentration: 0-5 μM Incubation Time: 72 hours Result: Showed high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines. Western Blot Analysis Cell Line: HCT116 cells [1] Concentration: 0.001, 0.01, 0.1, 1 and 10 μM Incubation Time: 4 and 24 hours Result: Inhibited the phosphorylation of FAK and its downstream proteins from multiple pathways. Cell Cycle Analysis Cell Line: HCT116 cells [1] Concentration: 0.01, 0.05, 0.1 and 0.5 μM for 24 hours; 0.01, 0.05, 0.1, 0.3 and 1 μM for 48 hours Incubation Time: 24 and 48 hours Result: Induced strong cell cycle arrest at the G2/M phase and apoptosis.

FAK-IN-2 (5 and 15 mg/kg; 16 days; once daily) has potent antitumor effects in model mice with a dose-dependent manner without significant toxicity [1] Pharmacokinetic Parameters of FAK-IN-2 in male Sprague-Dawley rats [1]. PO (5 mg/kg) IV (5 mg/kg) C max (μg/L) 239.87 2965.27 T max (h) 1.44 0.08 T 1/2 (h) 4.70 7.57 Clz (L/h/kg) 9.92 2.19 AUC 0-t (μg*h/L) 512.75 2439.06 F % 21.02% Animal Model: Female Balb/C nu/nu mice (HCT116-injected) [1] Dosage: 5 and 15 mg/kg Administration: 16 days; once daily Result: Displayed potent antitumor effects in a dose-dependent manner without significant toxicity.

C28H31ClN8O3

563.05

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years