Vorasidenib CAS# 1644545-52-7 PVM/MA共聚物
Vorasidenib, also known as AG-881, is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity. AG-881 specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations.
📌 参考资料/链接:
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of GliomaBy: Konteatis, Zenon; et alACS Medicinal Chemistry Letters (2020), 11(2), 101-107
📄 详细内容
CAS No. 1644545-52-7 PVM/MA共聚物Vorasidenib synthetic routes

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of GliomaBy: Konteatis, Zenon; et alACS Medicinal Chemistry Letters (2020), 11(2), 101-107
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