Quizartinib

Quizartinib (AC220) is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer^[1][2]. IC50 & Target:Kd: 1.6±0.7 nM (Flt3)^[1] In Vitro: Quizartinib (0-10,000 nM; 48 h) potently inhibits proliferation of leukemia cell lines dependent on FLT3^ITD, FIP1L1-PDGFRA, or select KIT mutations (V560G, N822K, D814Y) with IC₅₀ values ranging from <1 nM to 77 nM^[1].
Quizartinib (0-10,000 nM; 48 h) potently inhibits proliferation and induces apoptosis in isogenic Ba/F3 cells expressing FLT3^WT, FLT3^ITD, FLT3^K663Q, FLT3^D835Y, KIT^WT, or KIT^D816Y with IC₅₀ values ranging from <1 nM to 474 nM^[1].
Quizartinib (0-1000 nM; 90 min) selectively inhibits autophosphorylation of mutant KIT^D816Y, KIT and FLT3^ITD, FLT3^D835Y isoforms in isogenic Ba/F3 cells, while KIT^D816V and FLT3^D835V are largely resistant to dephosphorylation^[1].
Quizartinib (0-5000 nM; 48 h) inhibits proliferation of native AML blasts with wild-type KIT, FLT3 amplification, or select FLT3 ITD mutations, while FLT3 ITD-beta1-positive blasts are insensitive^[1].