Enasidenib is an inhibitor of mutant isocitrate dehydrogenase 2 (IDH2, IC50 = 0.1 µM for IDH2 R140Q). It is selective for IDH2 R140Q over wild-type IDH2, wild-type IDH1, and IDH1 R132H (IC50s = 1.8, 0.45, and 48.4 µM, respectively). Enasidenib (0.1, 1, and 5 µM) inhibits production of D-2-hydroxyglutarate...

Soluble in DMSO. Enasidenib, also known as AG221, is a potent and selective IDH2 mutant enzyme inhibitor. It caused a significant decrease in R(-)-2-hydroxyglutarate in marrow, plasma, and urine and showed a dose-dependent survival benefit in a primary human AML xenograft model carrying the IDH2 R140Q mutation....