纯度:98% by HPLC,;NMR (Conforms)
分子式:C27H31FN4O2
分子量:462.56
溶剂:DMSO (10 mg/ml) Ethanol (5 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):R132 mutant isocitrate dehydrogenase inhibitor
Function / Pharmacology:AGI-5198 is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1).1 It is selective for the R132H-IDH1 mutant and does not affect wild type cells.2 This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) form alpha-ketoglutarate (2-OG).