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Figure 2 | Molecular Cancer

Figure 2

From: Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms

Figure 2

Quizartinib potently induces apoptosis in selected leukemia cell line models. Leukemia cell lines harboring FLT3, KIT or PDGFRA mutations were treated with various doses of quizartinib for 48 hours and induction of apoptosis was measured using an annexin V-based assay. Representative density plots indicating early phase apoptosis (annexin V-positive cells) or late phase apoptotic cells (propidium iodide positivity) fractions are shown in a quadrant density dot plot. Whereas the FLT3 ITD + cell line MOLM14 (A) and the mutant-KIT V560G + cell line HMC1.1 (B) reveal potent sensitivity in the lower nanomolar range, the sister cell line HMC1.2 (C), harboring an additional KIT D816V mutation, is insensitive towards quizartinib treatment. Data presented in the dose–response curves on the right represents the average mean of at least 3 separate experiments (each normalized to the untreated controls, which are set to zero). IC50s of all tested cell lines are provided in Table 2.

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