Enasidenib, Mutant isocitrate dehydrogenase 2 (IDH2) inhibitor

Product Details

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

Alternate Names: AG-221

Molecular Formula: C₁₉H₁₇F₆N₇O

Formula Weight: 473.38

CAS Number: 1446502-11-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Mutant isocitrate dehydrogenase 2 (IDH2) inhibitor

Functions

Enasidenib is a potent (IC50’s = 100 nM IDH2R140Q homodimer, 30 nM IDH2R140Q/WT heterodimer and 10 nM IDH2R172K/WT heterodimer) and selective inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).  It suppressed the production of the oncometabolite (R)-2-Hydroxyglutarate (a competitive inhibitor of αKG-dependent dioxygenases which leads to epigenetic dysregulation) and induced cellular differentiation in primary human IDH2 mutation-positive acute myeloid leukemia cells.  Recently approved for clinical use by the FDA.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)