BCR-ABL-IN-2

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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。

BCR-ABL-IN-2 

BCR-ABL-IN-2 是 BCR-ABL1 激酶的抑制剂，其对 ABL1native 和 ABL1T315I 的 IC50 值分别为 57 nM，773 nM。

BCR-ABL-IN-2

BCR-ABL-IN-2 Chemical Structure

CAS No. : 897369-18-5

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生物活性

BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.

IC50 & Target

IC50: 57 nM (ABL1native), 773 nM (ABL1T315I)[1].
体外研究
(In Vitro)

BCR-ABL-IN-2 (Compound 1) contains a urea moiety to allow a hydrogen bond with the conserved K271-E286 salt bridge of ABL1, a t-butyl moiety to bind into the hydrophobic spine at the third pocket position, and a 2,3-dichlorophenyl ring to stabilize the DFG-phenylalanine F382 in the Type II-out conformation. BCR-ABL-IN-2 exhibits an IC50 of 57 nM for ABL1native and an IC50 of 773 nM for ABL1T315I[1]. Despite ABL, BCR-ABL-IN-2 can also inhibit KDR, BRaf, p38 kinase with IC50s of 1.8 μM, 0.23 μM, 6.3 nM, 43 nM, respectively[2].

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

502.39

Formula

C24H25Cl2N5O3
CAS 号

897369-18-5
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]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011 Apr 12;19(4):556-68.

    [2]. ARYL SULFONOHYDRAZIDES. US 2008/0113967 A1.

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