Description
A potent and selective inhibitor of mutant IDH1 (IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively); reduces 2-HG production and inhibits growth of MCF-10A-IDH1R132H/+ cells in a concentration-dependent manner; reduces concentration of tumor 2-HG in an HCT116-IDH1R132H/+ mouse xenograft model (200 mg/kg); suppresses 2-HG production and reduces tumor progression in an HMEX2838-IDH1R132C patient-derived melanoma mouse xenograft model (300 mg/kg),
Formal name: (4R)-4-[(1S)-1-fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2′-(trifluoromethyl)[3,4′-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-2-oxazolidinone
Synonyms:
Molecular weight: 490.5
CAS: 1628805-46-8
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Metabolism||Research Area|Endocrinology & Metabolism
