1429179-07-6
1429179-07-6 结构式
基本信息
中文别名
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-异丙基恶唑烷-2-酮
英文别名
IDH889IDH-889
IDH889
IDH-889
IDH 889
物理化学性质
沸点589.5±60.0 °C(Predicted)
密度1.284±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)4.15±0.10(Predicted)
形态Solid
颜色White to off-white
应用领域
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.