纯度:98%,;NMR (Conforms)
分子式:C19H17F6N7O
分子量:473.38
溶剂:DMSO (25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):IDH2 inhibitor
Function / Pharmacology:Enasidenib is a potent (IC50’s = 100 nM IDH2R140Q homodimer, 30 nM IDH2R140Q/WT heterodimer and 10 nM IDH2R172K/WT heterodimer) and selective inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).1 It suppressed the production of the oncometabolite (R)-2-Hydroxyglutarate (a competitive inhibitor of αKG-dependent dioxygenases which leads to epigenetic dysregulation) and induced cellular differentiation in primary human IDH2 mutation-positive acute myeloid leukemia cells.1,2 Recently approved for clinical use by the FDA.