Quizartinib
Quizartinib is an anticancer chemotherapeutic compound that inhibits FMS-like tyrosine kinase 3 (FLT3), c-Kit, and PDGFR. Quizartinib is clinically used to treat acute myelogenous leukemia. In cellular models, quizartinib induces apoptosis and inhibits proliferation. This compound also inhibits ATP-binding cassette ABCG2, also known as breast cancer resistance protein. Quizartinib is supplied as a crystalline solid. Quizartinib is soluble in DMSO to 33 mg/mL, in water to <0.3 mg/ml, and in ethanol to <0.5 mg/ml. If Quizartinib needs to be stored long term, we recommend storing the solid Quizartinib and not storing the Quizartinib in solution due to potential loss of stability.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18956253
| Cas No. |
950769-58-1 |
|---|---|
| Purity |
≥98% |
| Formula |
C29H32N6O4S |
| Formula Wt. |
560.67 |
| IUPAC Name |
1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea |
| Synonym |
AC220, AC-220 |
| Appearance |
White to off white powder |
Ostronoff F, Estey E. The role of quizartinib in the treatment of acute myeloid leukemia. Expert Opin Investig Drugs. 2013 Sep 26. [Epub ahead of print]. PMID: 24070241.
Bhullar J, Natarajan K, Shukla S, et al. The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions. PLoS One. 2013;8(8):e71266. PMID: 23967177.
Kampa-Schittenhelm KM, Heinrich MC, Akmut F, et al. 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. Mol Cancer. 2013 Mar 7;12:19. PMID: 23497317.
Zarrinkar PP, Gunawardane RN, Cramer MD, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. 2009 Oct 1;114(14):2984-92. PMID: 19654408.
