Enasidenib

• Background :

  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.

• Conjugation :

  Unconjugated

• Buffer :

  White solid

• Storage Conditions :

  -20°C