Synonyms: AG-221 | CC-90007 | Idhifa®
enasidenib is an approved drug (FDA (2017))
Compound class:
Synthetic organic
Comment: Enasidenib (AG-221) is an orally available inhibitor of isocitrate dehygrogenase 2 (IDH2), that is approved as an antineoplastic agent. This compound is example 409 in patent US20130190287 A1 [1].
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Bioactivity Comments |
IC50 values for biochemical inhibition of IDH2 mutants R140Q and R172K are between 100-1000nM [1]. Inhibition of wild type IDH2 was not assessed as the wild type enzyme does not produce the oncometabolite, 2-hydroxyglutarate (2-HG). |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
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