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Description: Enasidenib (formerly known as AG-221 and CC-90007) is an oral, first-in-class, potent and selective inhibitor of IDH2 (Isocitrate dehydrogenase 2) with potential anticancer activity. Enasidenib inhibits mutant IDH2-mediated 2-HG production in vivo and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Enasidenib induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells, effects that are further enhanced by simultaneous inhibition of Flt3ITD. Clinical trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy.
References: Blood 2014 124:437; http://cancerres.aacrjournals.org/content/74/19_Supplement/3116
Related CAS#:1650550-25-6 (mesylate)
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