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Characteristics
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Cell-permeable. A second generation FLT3 receptor tyrosine kinase inhibitor. Quizartinib displays high affinity for FLT3 in a binding assay (kDa= 1.6 nM) and is a potent inhibitor in cellular autophosphorylation assays (IC50 = 1.1 nM for FLT3-ITD and 4.2 nM for wt FLT3). It inhibits the growth of human leukemia cell line MV4-11 (IC500 = 0.56 nM) which is FLT3 dependent and contains a homozygous FLT3-ITD mutation, and A375 cells (IC50 > 10,000 nM) which are not FLT3 dependent and contain an activating mutation in BRAF.
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