货号	规格	价格	上海	北京	珠海	重庆	武汉
V47546-1mg	≥98%	￥1810.00 V47546-1mg ￥1810.00 3-5天	0 货期：3-5天	-	-	-	-
V47546-5mg	≥98%	￥5440.00 V47546-5mg ￥5440.00 3-5天	0 货期：3-5天	-	-	-	-
V47546-10mg	≥98%	￥7180.00 V47546-10mg ￥7180.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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.

体外研究：

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.
FAK-IN-2 (0-30 nM; 14 days) can remarkably affect HCT-116 cells clone formation in a dose-dependent manner.
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.
FAK-IN-2 (0.001-10 μM; 4 and 24 hours) inhibits the phosphorylation of FAK and its downstream proteins from multiple pathways.
FAK-IN-2 (0.01-1 μM; 24 or 48 hours) induces strong cell cycle arrest at the G2/M phase and apoptosis.

体内研究：

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
Pharmacokinetic Parameters of FAK-IN-2 in male Sprague-Dawley rats.

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.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.776 ml	8.88 ml	17.76 ml
5 mM	0.355 ml	1.776 ml	3.552 ml
10 mM	0.178 ml	0.888 ml	1.776 ml
50 mM	0.036 ml	0.178 ml	0.355 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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