1395051-72-5
中文名稱
化合物 BPR1J-340
英文名稱
BPR1J-340
CAS
1395051-72-5
分子式
C29H34N8O3
分子量
542.63
MOL 文件
1395051-72-5.mol
1395051-72-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 BPR1J-340 英文別名
BPR1J-340N-(3-(4-[([(5-ethyl-3-isoxazolyl)amino]carbonylamino)methyl]phenyl)-1H-5-pyrazolyl)-4-[(4-methylpiperazino)methyl]benzamide
物理化學(xué)性質(zhì)
沸點716.2±60.0 °C(Predicted)
密度1.310±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)12.62±0.70(Predicted)
應(yīng)用領(lǐng)域
用途一
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.