BPR1J-097 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 11 nM).1 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.
1.Lin, W.-H., Jiaang, W.-T., Chen, C.-W., et al.BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AMLBr. J. Cancer106(3)475-481(2012)