CCT241736

Description	CCT241736 is a novel, orally bioavailable, imidazo[4,5-b]pyridine derivative discovered at our Institute, highly selective for FLT3 and Aurora kinases with an S(10) selectivity score using KINOMEscan™ technology of 0.057 (fraction of 386 non-mutant kinases inhibited >90% when screened at 1 uM of CCT241736; San Diego, CA).In biochemical kinase studies, CCT241736 has IC50 values against FLT3, Aurora A and Aurora B of 0.035, 0.015 and 0.1 uM respectively. Furthermore, CCT241736 inhibits a wide range of FLT3 mutants, including FLT3-ITD, -D835Y, -D835H, -K663Q and –N841I. In cellular assays, CCT241736 inhibits viability of the human FLT3-ITD positive AML cell lines MOLM-13 and MV-4-11 with EC50 values of 0.1 and 0.27 uM respectively.
Pathways	Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Epigenetics
Targets	Aurora FLT3

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