| Identification | Back Directory | [Name]
BPR1J-340 | [CAS]
1395051-72-5 | [Synonyms]
BPR1J-340
N-(3-(4-[([(5-ethyl-3-isoxazolyl)amino]carbonylamino)methyl]phenyl)-1H-5-pyrazolyl)-4-[(4-methylpiperazino)methyl]benzamide | [Molecular Formula]
C29H34N8O3 | [MOL File]
1395051-72-5.mol | [Molecular Weight]
542.63 |
| Hazard Information | Back Directory | [Description]
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. |
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