Enasidenib | Inhibitor of IDH2

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$45.00
25 mg$150.00

Enasidenib (1446502-11-9) 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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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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