c-Met-IN-12 | 赛默飞Alfa aesar官网

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。

c-Met-IN-12

c-Met-IN-12 (化合物 4r) 是一种口服有效和选择性的 II 型 c-Met 激酶抑制剂，其 IC₅₀ 值为 10.6 nM。c-Met-IN-12 对 AXL、Mer 和TYRO3 激酶表现出较高的抑制作用 (1 μM 抑制率 > 80%)。c-Met-IN-12 可作为一种支架进一步增强激酶选择性。c-Met-IN-12具有抗肿瘤作用。

c-Met-IN-12 Chemical Structure

CAS No. : 2426675-70-7

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生物活性

c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC₅₀ of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy^[1].

IC₅₀ & Target

c-Met

10.6 nM (IC₅₀)

体内研究
(In Vivo)

c-Met-IN-12 (compound 4r) (Tumor-bearing nude mice, 45 mg/kg, Orally, Q.D. for 21 days) exhibits significant tumor growth inhibition (93%) in a U-87MG human gliobastoma xenograft model^[1].

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

分子量

576.62

Formula

C₃₄H₂₉FN₄O₄

CAS 号

2426675-70-7

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]. Xu H, et al. Discovery of N-substituted-3-phenyl-1,6-naphthyridinone derivatives bearing quinoline moiety as selective type II c-Met kinase inhibitors against VEGFR-2. Bioorg Med Chem. 2020 Jun 15;28(12):115555.

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