CCT241736
CAS号 | 1402709-93-6 | 货号 | BCP29563 |
中文名 | CCT241736 | ||
英文名 | CCT241736 | ||
中文别名 | |||
英文别名 | CCT 241736;CCT-241736; | ||
分子式 | C22H23Cl2N7 | 分子量 | 456.37 |
生物活性 | 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. | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Epigenetics | ||
靶 点 | Aurora FLT3 |
结构式
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