CHMFL-ABL-121

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。

CHMFL-ABL-121 

CHMFL-ABL-121 是一种 II 型 ABL 激酶高效抑制剂，抑制纯化的非活性 ABL wt 和 T315I 激酶蛋白的 IC50 值分别为 2 nM 和 0.2 nM。

CHMFL-ABL-121

CHMFL-ABL-121 Chemical Structure

CAS No. : 2270879-07-5

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生物活性

CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively[1].

IC50 & Target[1]

ABL wt

2 nM (IC50)

ABL-T315I

0.2 nM (IC50)

体外研究
(In Vitro)

CHMFL-ABL-121 dose-dependently inhibits BCRABL’s auto-phosphorylation at Y245 site in K562 (EC50<10 nm), meg-01 (ec50<10 nm) and ku812 (ec50<30 nm) cells and also significantly blocks the phosphorylation of downstream signaling mediators stat5, crkl erk[1].
CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

580.67

Formula

C30H31F3N6OS
CAS 号

2270879-07-5
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 X, et al. Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81.

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