enasidenib
Ligand Summary
Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells.
UNII: 3T1SS4E7AG
PubChem: 89683805
PubChem: 90480031
ChEMBL: CHEMBL3989908
ChEMBL: CHEMBL3989931
DrugCentral: 5251
LyCHI: PKNY8FA8JK8L
Target Activities
10 Activities
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