Enasidenib (1446502-11-9) Description:
Enasidenib, aslo known as AG-221 and CC-90007, 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.
Enasidenib is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, enasidenib specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG.
Enasidenib (1446502-11-9) Specifications:
|Product Name||Enasidenib (AG-221)|
|Synonyms||AG-221; AG 221; AG221; CC-90007; CC 90007; CC90007; Enasidenib|
|Purity||>98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||473.14 g/mol|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||Enasidenib is a first-in-class oral selective inhibitor of mutant IDH2 enzymes (isocitrate dehydrogenase 2), for the treatment of adults with relapsed or refractory IDH2-mutated acute myeloid leukemia.|