BPR1J-097

Research use only, not for human use.

BPR1J-097 is a novel FLT-3 inhibitor(IC50: 11±7 nM) with promising in vivo anti-tumor activities. It also inhibits FLT-3 D835Y (IC50: 3 nM).

BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities. BPR1J-097 may be useful in AML treatments.IC50 of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21±7 and 46±14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models.

BPR1J097; BPR1J-097; BPR1J 097

Angiogenesis

EGFR

FLT3

Cancer

——

1327167-19-0

516.62

C27H28N6O3S

98%

——

CN1CCN(CC1)c1ccc(cc1)C(=O)Nc1n[nH]c(c1)c1cc(ccc1)NS(=O)(=O)c1ccccc1

4-(4-methylpiperazin-1-yl)-N-(3-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-5-yl)benzamide.

(-20℃)

With Ice Pack

≥ 2 years