A selective inhibitor of IDH2; reduces 2-hydroxyglutarate levels

Enasidenib – 5 mg

Brand:
Cayman
CAS:
1446502-11-9
Storage:
-20
UN-No:
Non-Hazardous - /

Enasidenib is an orally available, allosteric inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).{33576,33575} It displays selectivity for mutant IDH2 over wild-type IDH2, wild-type IDH1, mutant IDH1, and a panel of kinases.{33575} Studies in primary human mutant IDH2-positive acute myeloid leukemia (AML) cells ex vivo and xenograft mouse models have shown that enasidenib can reduce 2-hydroxyglutarate levels, reverse histone and DNA hypermethylation, and promote cellular differentiation.{33576,33575} In clinical trials, it has been shown to induce hematological responses in patients with mutant IDH2 AML.{33576}  

 

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Description

A selective inhibitor of IDH2; reduces 2-hydroxyglutarate levels, reverses histone and DNA hypermethylation, and promotes cellular differentiation in primary human mutant IDH2-positive AML cells ex vivo and xenograft mouse models

Formal name: 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-pyridinyl]amino]-1,3,5-triazin-2-yl]amino]-2-propanol

Synonyms:  AG-221|CC-90007

Molecular weight: 473.4

CAS: 1446502-11-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Metabolism

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