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 IDH1 R132* 突變型具有高效選擇性，對 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。