Description
An inhibitor of mutant IDH (IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively); inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively); decreases the production of 2-HG in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively); reduces tumor growth in a TS603-IDH1R132H mouse xenograft model at 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
Synonyms: AG-881
Molecular weight: 414.7
CAS: 1644545-52-7
Purity: ≥98%
Formulation: A crystalline solid