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BCR-ABL-IN-2
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BCR-ABL-IN-2图片
CAS NO:897369-18-5
包装与价格：
包装价格(元)
250mg电议
500mg电议

产品介绍
BCR-ABL-IN-2是BCR-ABL1激酶的抑制剂，其对ABL1native和ABL1T315I的IC50值分别为57nM，773nM。
Cas No.897369-18-5
Canonical SMILESO=C([C@H]1NCC2=C(C=C(N3N=C(C(C)(C)C)C=C3NC(NC4=CC=CC(Cl)=C4Cl)=O)C=C2)C1)O
分子式C24H25Cl2N5O3
分子量502.39
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

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].

[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.