BPR1J-097

BPR1J-097 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3, IC50 = 11 nM). It is selective for FLT3 over FLT1, KDR, Aurora A, and Aurora B kinases (IC50s = 211, 129, 340, and 876 nM, respectively). BPR1J-097 inhibits FLT3 activity and phosphorylation of STAT5 in MV4-11 acute myeloid leukemia (AML) cells containing the FLT3 activating mutant FLT3-ITD (IC50s = 10 and 1 nM, respectively). It inhibits the growth of FLT3-dependent MOLM-13 and MV4-11 AML cells (GI50s = 21 and 46 nM, respectively) but not FLT3-/- U937 and K562 cells (GI50s = >20,000 nM for both). BPR1J-097 (25 mg/kg) inhibits tumor growth in a MOLM-13 mouse xenograft model.Formal Name: 4-(4-methyl-1-piperazinyl)-N-[5-[3-[(phenylsulfonyl)amino]phenyl]-1H-pyrazol-3-yl]-benzamide. CAS Number: 1327167-19-0. Molecular Formula: C27H28N6O3S. Formula Weight: 516.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:6): 0.14 mg/ml, DMSO: 10 mg/ml. lambdamax: 298 nm. SMILES: CN1CCN(C2=CC=C(C(NC3=NNC(C4=CC(NS(C5=CC=CC=C5)(=O)=O)=CC=C4)=C3)=O)C=C2)CC1. InChi Code: InChI=1S/C27H28N6O3S/c1-32-14-16-33(17-15-32)23-12-10-20(11-13-23)27(34)28-26-19-25(29-30-26)21-6-5-7-22(18-21)31-37(35,36)24-8-3-2-4-9-24/h2-13,18-19,31H,14-17H2,1H3,(H2,28,29,30,34). InChi Key: RRKKHABFIOHAOI-UHFFFAOYSA-N.