BPR1J-340 - CAS 1395051-72-5

BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD (+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibition and regression in FLT3-ITD (+) AML murine xenograft models. The combination treatment of the HDAC inhibitor vorinostat (SAHA) with BPR1J-340 synergistically induced apoptosis via Mcl-1 down-regulation in MOLM-13 AML cells, indicating that the combination of selective FLT3 kinase inhibitors and HDAC inhibitors could exhibit clinical benefit in AML therapy.

Apoptosis, FLT, Others

Angiogenesis, Tyrosine Kinase/Adaptors, Others, Apoptosis

1394974

C29H34N8O3

542.63

N(C(=O)C1=CC=C(CN2CCN(C)CC2)C=C1)C=3C=C(NN3)C4=CC=C(CNC(NC=5C=C(CC)ON5)=O)C=C4

-20°C

Ice Packs

Small Compound