Enasidenib

Enasidenib

【产品别名】AG-221

【CAS号】 1446502-11-9

【目录编号】 2H-54

【纯度】 99.76%

【分子式】 C19H17F6N7O

【分子量】 473.38

【简介】 Enasidenib is a oral potent, selective, reversible inhibitor of mutant IDH2.

联系我们 索取资料

Enasidenib 详细介绍

Enasidenib is a oral potent, selective, reversible inhibitor of mutant IDH2.
Target: IDH2
in vitro: Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer . The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer.
in vivo: AG-221 is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. In an updated analysis of a dose-ecalation phase I trial that now includes 73 patients with advanced hematologic cancer, AG-221 was well tolerated and achieved more than 90% inhibition of its target (ie, 2-HG [2-hydroxyglutarate]) in patients with an IDH2mutation.

Back to top