Quizartinib CAS# 950769-58-1 奎扎替尼

Quizartinib (AC220) is a potent, selective FLT3 inhibitor with sub-nanomolar biochemical potency (FLT3 ITD IC₅₀ ≈ 1–2 nM) and >10-fold selectivity over most kinases. In FLT3-ITD–positive AML cell lines, it inhibited FLT3 phosphorylation and downstream STAT5/ERK signaling with cellular IC₅₀ values of ~1–10 nM, inducing apoptosis and suppressing proliferation. In MV4-11 xenograft mouse models, oral quizartinib produced rapid tumor regression and prolonged survival at doses as low as 1–10 mg/kg. It also reduced leukemic burden in FLT3-ITD knock-in mouse models. Pharmacokinetic studies showed good oral bioavailability and sustained plasma exposures supporting continuous target inhibition and advancement to clinical testing.