BCR-ABL-IN-2 |
| Katalog-Nr.GC33368 |
BCR-ABL-IN-2 ist ein Inhibitor der BCR-ABL1-Tyrosinkinase mit IC50-Werten von 57 nM, 773 nm fÜr ABL1native bzw. ABL1T315I.
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Cas No.: 897369-18-5
Sample solution is provided at 25 µL, 10mM.
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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.
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