An inhibitor of mutant IDH2
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Enasidenib

Item No. 21277

Technical Information
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
CAS Number
1446502-11-9
Synonyms
  • AG-221
  • CC-90007
Molecular Formula
C19H17F6N7O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
λmax
237, 272 nm
SMILES
CC(C)(O)CNC1=NC(NC2=CC=NC(C(F)(F)F)=C2)=NC(C3=CC=CC(C(F)(F)F)=N3)=N1
InChi Code
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)
InChi Key
DYLUUSLLRIQKOE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Enasidenib is an inhibitor of mutant isocitrate dehydrogenase 2 (IDH2; IC50 = 0.1 µM for IDH2 R140Q).1 It is selective for IDH2 R140Q over wild-type IDH2, wild-type IDH1, and IDH1 R132H (IC50s = 1.8, 0.45, and 48.4 µM, respectively). Enasidenib (0.1, 1, and 5 µM) inhibits production of D-2-hydroxyglutarate (Item No. 11605) and induces differentiation in primary acute myeloid leukemia (AML) cells expressing IDH2 R140Q. It increases survival in a patient-derived xenograft (PDX) mouse model when administered at doses of 5, 15, and 45 mg/kg. Formulations containing enasidenib have been used in the treatment of AML.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yen, K., Travins, J., Wang, F., et alAG-221, a first-in-class therapy targeting acute myeloid leukemia harboring oncogenic IDH2 mutations. Cancer Discov. 7(5), 478-493 (2017).