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Product Details

Enasidenib | Inhibitor of IDH2

Enasidenib (1446502-114-9) 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).1  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.1,2  Recently approved for clinical use by the FDA.

References/Citations

1) Yen et al. (2017), AG-221, A First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations; Cancer Discov. 7 478
2) Amatangelo et al. (2017), Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response; Blood 130 732

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Catalog#  10-4660-0005

$55.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1446502-11-9
Catalog Number:
10-4660
Activity:
Inhibitor of IDH2
Chemical 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 Weight:
473.38
Molecular Formula:
C19H17F6N7O
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
98%
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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