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57nM，773nM。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx13028
- CAS: 897369-18-5
- 别名:
- 分子式: C24H25Cl2N5O3
- 分子量: 502.39
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
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.
