ALK/ROS1-IN-1

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。

ALK/ROS1-IN-1 

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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生物活性

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]
体外研究
(In Vitro)

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

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

584.63

Formula

C30H35F3N6O3
CAS 号

2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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