G-749

G-749 is an inhibitor of Fms-like tyrosine receptor kinase 3 (FLT3) with IC50 values ranging from 2.1 to 38.1 nM for wild-type and mutant (constitutively active) FLT3s in Ba/F3 cells expressing recombinant receptors. It also inhibits growth of human leukemia cell lines that express FLT3-ITD mutant kinase (IC50s = 3.5 and 7.5 nM for MV4-11 and Molm-14 cells, respectively) but has no effect on cells that lack FLT3 expression or that express wild-type FLT3. G-749 reduces tumor growth and increases survival in a dose-dependent manner in MV4-11 and Molm-14 murine leukemia xenograft models. It reduces growth of bone marrow blasts derived from acute myeloid leukemia patients, showing more potent inhibition of blasts expressing the FLT3-ITD mutant receptor.Formal Name: 8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]-pyrido[4,3-d]pyrimidin-5(6H)-one. CAS Number: 1457983-28-6. Molecular Formula: C25H25BrN6O2. Formula Weight: 521.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 3 mg/ml. lambdamax: 261 nm. SMILES: BrC1=CNC(C2=C1N=C(NC3CCN(C)CC3)N=C2NC4=CC=C(OC5=CC=CC=C5)C=C4)=O. InChi Code: InChI=1S/C25H25BrN6O2/c1-32-13-11-17(12-14-32)29-25-30-22-20(26)15-27-24(33)21(22)23(31-25)28-16-7-9-19(10-8-16)34-18-5-3-2-4-6-18/h2-10,15,17H,11-14H2,1H3,(H,27,33)(H2,28,29,30,31). InChi Key: SXWMIXPJPNCXQQ-UHFFFAOYSA-N.