Enasidenib

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 (Cay-11605) and induces differentiation in primary acute myeloid leukemia (AML) cells expressing IDH2 R140Q. It increases survival in a patient-derived xenograft (PDX) mouse model when administered at doses of 5, 15, and 45 mg/kg. Formulations containing enasidenib have been used in the treatment of AML.Formal Name: 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-pyridinyl]amino]-1,3,5-triazin-2-yl]amino]-2-propanol. CAS Number: 1446502-11-9. Synonyms: AG-221, CC-90007. Molecular Formula: C19H17F6N7O. Formula Weight: 473.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 10 mM. lambdamax: 237, 272 nm. SMILES: CC(C)(O)CNC1=NC(NC2=CC=NC(C(F)(F)F)=C2)=NC(C3=CC=CC(C(F)(F)F)=N3)=N1. InChi Code: InChI=1S/C19H17F6N7O/c1-17(2,33)9-27-15-30-14(11-4-3-5-12(29-11)18(20,21)22)31-16(32-15)28-10-6-7-26-13(8-10)19(23,24)25/h3-8,33H,9H2,1-2H3,(H2,26,27,28,30,31,32). InChi Key: DYLUUSLLRIQKOE-UHFFFAOYSA-N.