BCR-ABL-IN-2,897369-18-5

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BCR-ABL-IN-2

CAS No. : 897369-18-5

MCE 国际站：BCR-ABL-IN-2

产品活性：BCR-ABL-IN-2 是 BCR-ABL1 激酶的抑制剂，其对 ABL1^native 和 ABL1^T315I 的 IC₅₀ 值分别为 57 nM，773 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Bcr-Abl

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 ABL1^native and an IC₅₀ of 773 nM for ABL1^T315I. 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.

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