1429179-07-6
1429179-07-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15551(S)-3-(2-(((S)-1-(5-(4-氟-3-甲基苯基)嘧啶-2-基)乙基)氨基)嘧啶-4-基)-4-異丙基惡唑烷-2-酮
英文別名
IDH889IDH-889
IDH889
IDH-889
IDH 889
物理化學(xué)性質(zhì)
沸點(diǎn)589.5±60.0 °C(Predicted)
密度1.284±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.15±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM. IDH889 demonstrates significantly improved plasma exposure in mice vs IDH662 (AUC 3.6 μM·h, Cmax 1.7 μM at 10 mg/kg; AUC 55.5 μM·h, Cmax 14.2 μM at 100 mg/kg). IDH889 also has excellent permeability and no efflux in the Caco-2 and human MDR1-MDCK cell lines, supporting the hypothesis that potent inhibition of mutant IDH1 function by binding at the allosteric binding site is compatible with brain penetration.常見問題列表
概述
IDH889 是一種可口服利用的，腦滲透性的，變構(gòu)和突變特異性的異檸檬酸脫氫酶 (IDH1) 抑制劑。IDH889 對(duì) IDH1 R132* 突變型具有高效選擇性，對(duì) IDH1R132H、IDH1R132C 和 IDH1wt 作用的 IC50 值分別為 0.02 μM, 0.072 μM 和 1.38 μM。IDH889 具有高效的細(xì)胞內(nèi) 2-HG 水平抑制作用，其 IC50 值為 0.014 μM。