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AG-221

 - Enasidenib
Axon 2745
Based on 15 publications in PubMed
CAS:  1446502-11-9
Purity:  99%
  • Soluble in DMSO
  • MF:  C19H17F6N7O
  • MW:  473.37

Description

AG-221 (enasidenib) is an orally active, selective inhibitor of oncogenic mutant isocitrate dehydrogenase 2 (IDH2), with a reported IC50 value of 100 nM. It inhibits neomorphic mutant-IDH2 activity and reduces production of the oncometabolite D-2-hydroxyglutarate (2-HG).

Suppression of 2-HG by AG-221 relieves the differentiation block associated with IDH2 mutations and promotes maturation of mutant hematopoietic cells. It is used to study mutant-IDH2 enzymology, oncometabolite signaling and differentiation responses in primary AML samples and xenograft models.

Key Features

  • Orally bioavailable and selective mutant-IDH2 inhibitor
  • IC50: 100 nM
  • Suppresses D-2-hydroxyglutarate production
  • Promotes differentiation of IDH2-mutant cells

Applications

  • Mutant IDH2 research
  • 2-HG quantification assays
  • AML differentiation studies
  • Cancer-metabolism research
  • IDH2-mutant xenograft models

More Information

Parent CAS No. 1446502-11-9
Chemical Name 2-Methyl-1-(4-(6-(trifluoromethyl)pyridin-2-yl)-6-(2-(trifluoromethyl)pyridin-4-ylamino)-1,3,5-triazin-2-ylamino)propan-2-ol
SMILES N1C(C(F)(F)F)=CC(NC2N=C(C3C=CC=C(C(F)(F)F)N=3)N=C(NCC(C)(C)O)N=2)=CC=1
MFCD N.A.
InChi InChI=1S/C19H17F6N7O/c1-17(2,33)9-27-15-30-14(11-4-3-5-12(29-11)18(20,21)22)31-16(32-15)28-10-6-7-26-13(8-10)19(23,24)25/h3-8,33H,9H2,1-2H3,(H2,26,27,28,30,31,32)
InChiKey DYLUUSLLRIQKOE-UHFFFAOYSA-N
CID 89683805
Short Description IDH2 inhibitor

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