Quizartinib (AC220) stands out as a highly effective agent in targeted cancer therapy, particularly for Acute Myeloid Leukemia (AML). Understanding its chemical characteristics and experimental performance is crucial for researchers and clinicians alike. This article details the chemical properties of Quizartinib and summarizes its in vitro and in vivo activity.

Chemically, Quizartinib is defined by its complex molecular structure, with the IUPAC name N-[5-(1,1-Dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]urea. Its molecular formula is C29H32N6O4S, and its molar mass is approximately 560.67 g/mol. These properties influence its solubility and formulation, with it typically appearing as a white or off-white crystalline powder. Its solubility is highest in DMSO, facilitating its use in in vitro assays.

In vitro studies have extensively characterized Quizartinib's potency and selectivity. Its primary target, FLT3, is inhibited with remarkable affinity, demonstrating very low IC50 values (often in the low nanomolar range) for FLT3-ITD mutated cell lines such as MV4-11. This potent inhibition leads to decreased leukemic cell proliferation and, critically, the induction of apoptosis. Unlike less selective inhibitors, Quizartinib shows minimal activity against a wide panel of other kinases, highlighting its targeted approach.

The in vivo performance of Quizartinib has been equally impressive. Preclinical studies using mouse models of FLT3-ITD driven AML have shown that oral administration of Quizartinib can lead to significant tumor regression and prolonged survival. These studies confirm its ability to inhibit FLT3 autophosphorylation within the tumor microenvironment and effectively halt disease progression. The research data, often sourced from chemical suppliers, provides crucial guidance on in vivo formulation and dosing strategies.

The consistent efficacy demonstrated in both in vitro and in vivo settings underscores Quizartinib's potential as a therapeutic agent. The availability of high-quality Quizartinib through specialized suppliers supports ongoing research, enabling scientists to further probe its complex interactions within cellular systems and animal models, and to refine its application in clinical settings.