Quizartinib

Quizartinib is an inhibitor of FMS-related tyrosine kinase 3 (FLT3, Kd = 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases. It inhibits the proliferation of the human leukemia cell line MV4-11, which harbors a homozygous FLT3-ITD mutation, with an IC50 value of 0.56 nM. At 1 mg/kg/day, quizartinib has been shown to extend survival in a mouse model of FLT3-ITD acute myeloid leukemia and to eradicate tumors in an FLT3-dependent mouse xenograft model at 10 mg/kg.Formal Name: N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]-urea. CAS Number: 950769-58-1. Synonyms: AC220. Molecular Formula: C29H32N6O4S. Formula Weight: 560.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 295 nm. SMILES: O=C(NC1=NOC(C(C)(C)C)=C1)NC2=CC=C(C3=CN4C(SC5=C4C=CC(OCCN6CCOCC6)=C5)=N3)C=C2. InChi Code: InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36). InChi Key: CVWXJKQAOSCOAB-UHFFFAOYSA-N.