Chemical Structure : CCT245718
货号: PC-72759Not For Human Use, Lab Use Only.
CCT245718 is a potent, dual Aurora A/FLT3 inhibitor with Kd of 39 nM (FLT3 D835Y) and 170 nM (FLT3 ITD), IC50 of 15 nM (Aurora A).
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CCT245718 is a potent, dual Aurora A/FLT3 inhibitor with Kd of 39 nM (FLT3 D835Y) and 170 nM (FLT3 ITD), IC50 of 15 nM (Aurora A).
CCT245718 weakly inhibits Aurora B with IC50 of 3045 nM.
CCT245718 exhibits potent antiproliferative activity towards FLT3-ITD + AML cell lines and strongly binds to FLT3-ITD and TKD (D835Y) mutants in vitro.
CCT245718 reduces phosphorylation of STAT5, downregulation of survivin and induces apoptotic cell death.
CCT245718 overcomes TKD-mediated resistance in a MOLM-13-derived cell line containing FLT3 with both ITD and D835Y mutations.
分子量 | 436.900 | |
分子式 | C22H21ClN6O2 | |
外观性状 | Solid | |
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1. Tariq MU, et al. Br J Cancer. 2021 Sep;125(7):966-974.
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