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

基本信息物理化學(xué)性質(zhì) 應(yīng)用領(lǐng)域常見問題列表

基本信息

中文別名

化合物 BPR1J-340

英文別名

BPR1J-340
N-(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.

常見問題列表

概述

BPR1J-340 是一種強效的 FLT3 抑制劑，IC50 約為 25 nM。BPR1J-340 可抑制 FLT3 和 STAT5 的磷酸化，并引發(fā) FLT3-ITD+ 急性髓系白血病 (AML) 細胞凋亡 (apoptosis)。BPR1J-340 表現(xiàn)出顯著的抗腫瘤活性。