Vorasidenib

Vorsidenib is an inhibitor of mutant isocitrate dehydrogenase (IDH, IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively). It also inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively). Vorsidenib decreases the production of D-2-hydroxyglutarate (2-HG, Cay-25895, Cay-11605) in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively). It reduces tumor growth in a TS603-IDH1R132H mouse xenograft model when administered at a dose of 50 mg/kg.Formal Name: 6-(6-chloro-2-pyridinyl)-N2,N4-bis[(1R )-2,2,2-trifluoro-1-methylethyl]-1,3,5-triazine-2,4-diamine. CAS Number: 1644545-52-7. Synonyms: AG-881. Molecular Formula: C14H13ClF6N6. Formula Weight: 414.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 218, 284 nm. SMILES: ClC1=NC(C2=NC(N[C@H](C)C(F)(F)F)=NC(N[C@H](C)C(F)(F)F)=N2)=CC=C1. InChi Code: InChI=1S/C14H13ClF6N6/c1-6(13(16,17)18)22-11-25-10(8-4-3-5-9(15)24-8)26-12(27-11)23-7(2)14(19,20)21/h3-7H,1-2H3,(H2,22,23,25,26,27). InChi Key: QCZAWDGAVJMPTA-UHFFFAOYSA-N.