Enasidenib is a potent (IC50s = 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 alphaKG-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.
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