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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 oral, selective, first-in-class inhibitor of the mutant IDH2 enzyme (IC50 value of 100 nM). AG-221 demonstrates excellent pharmaceutical properties, including adequate solubility, low clearance, and good oral bioavailability, and potently inhibits 2HG production by both the IDH2R140Q/WT heterodimer and IDH2R140Q homodimer. AG-221 suppressed 2HG production and induced cellular differentiation in primary human IDH2 mutation–positive acute myeloid leukaemia (AML) cells ex vivo and in xenograft mouse 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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