IDH305 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively).
CAS：1628805-46-8
分子式：C23H22F4N6O2
分子量：490.5
纯度：98%
存储：Store at -20°C

Background:

IDH305 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively). It reduces R-2-hydroxyglutarate (2-HG) production, a marker of mutant IDH1 activity, and inhibits growth of MCF-10A-IDH1R132H/+ cells in a concentration-dependent manner but has no effect on HCT116 cells expressing mutant IDH2. IDH305 (200 mg/kg) reduces the concentration of tumor 2-HG in an HCT116-IDH1R132H/+ mouse xenograft model. It also suppresses 2-HG production and reduces tumor progression in an HMEX2838-IDH1R132C patient-derived melanoma mouse xenograft model when administered at a dose of 300 mg/kg.