Gilteritinib

Gilteritinib is an inhibitor of FMS-related tyrosine kinase 3 (FLT3, IC50 = 5 nM for the wild-type enzyme). It inhibits mutant forms of FLT3, including FLT3 with the internal tandem duplication mutation (FLT3-ITD), FLT3-ITD expressing the F691L mutation, and FLT3 with various tyrosine kinase domain mutations (FLT3-TKD, IC50s =1.4-1.8, 12.2, and 0.7-2 nM, respectively). Gilteritinib also inhibits Axl and c-Kit with IC50 values of 41 and 102 nM, respectively. It decreases the viability of blast cells isolated from patients with relapsed acute myeloid leukemia (AML) in a concentration-dependent manner. Formulations containing gilteritinib have been used in the treatment of AML.Formal Name: 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-2-pyrazinecarboxamide. CAS Number: 1254053-43-4. Synonyms: ASP2215. Molecular Formula: C29H44N8O3. Formula Weight: 552.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml, Ethanol: 20 mg/ml. lambdamax: 213, 314, 366 nm. SMILES: CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5CCOCC5)=C(CC)N=C4C(N)=O)C=C3OC)CC2)CC1. InChi Code: InChI=1S/C29H44N8O3/c1-4-23-28(31-20-9-17-40-18-10-20)34-29(26(33-23)27(30)38)32-21-5-6-24(25(19-21)39-3)37-11-7-22(8-12-37)36-15-13-35(2)14-16-36/h5-6,19-20,22H,4,7-18H2,1-3H3,(H2,30,38)(H2,31,32,34). InChi Key: GYQYAJJFPNQOOW-UHFFFAOYSA-N.