Vorasidenib
Isocitrate dehydrogenase (IDH) 1/2 inhibitor / Vorasidenib is a highly potent (IC50’s = 7 nM IDH2-R140Q, 0.6 nM IDH1-R132H/WT, and 0.25 nM Neurosphere TS603 IDH1-R132H), selective, and brain-penetrant inhibitor of mutant isocitrate dehydrogenase 1 and 2 (IDH1/2).1 It led to >97% inhibition of 2-hydroxyglutarate production in mIDH1 glioma tissue. Vorasidenib significantly improved progression-free survival and delayed time to next intervention in a phase 3 glioma trial.2
Biochemicals & reagents
1644545-52-7
AG-881
1) Konteatis et al. (2020), Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma; ACS Med. Chem. Lett. 11 101 2) Mellinghoff et al. (2023), Vorasidenib in IDH1- or IDH2-Mutant Low-Grade Glioma; N. Engl. J. Med. 389 589
-20°C
TARGET: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH); Energy production -- PATHWAY: Mitochondrial function; NAD, NADP pathways -- DISEASE AREA: Cancer