AG-221 (Enasidenib) is an oral, selective, first-in-class inhibitor of the mutant IDH2 enzyme (IC50 value of 100 nM). AG-221 demonstrates excellent pharmaceutical properties, including adequate solubility, low clearance, and good oral bioavailability, and potently inhibits 2HG production by both the IDH2R140Q/WT heterodimer and IDH2R140Q homodimer. AG-221 suppressed 2HG production and induced cellular differentiation in primary human IDH2 mutation–positive acute myeloid leukaemia (AML) cells ex vivo and in xenograft mouse models.

KEYWORDS: AG-221 | supplier | IDH2 inhibitor | Enasidenib | AG 221 | AG221 | CAS [1446502-11-9] | Isocitrate | IDH | Inhibitor | Enzymes