FAK-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FAK-IN-2 

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 (FAK IC50= 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

FAK-IN-2 Chemical Structure

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生物活性

FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 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].

IC50 & Target

IC50: 35 nM (FAK)[1]
体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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)
Cmax (μg/L) 239.87 2965.27
Tmax (h) 1.44 0.08
T1/2 (h) 4.70 7.57
Clz (L/h/kg) 9.92 2.19
AUC0-t (μg*h/L) 512.75 2439.06
F % 21.02%

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

563.05

Formula

C28H31ClN8O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chen T, et al. Design, synthesis, and biological evaluation of novel covalent inhibitors targeting focal adhesion kinase. Bioorg Med Chem Lett. 2021;54:128433.

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