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Gamma Secretase

Enasidenib (1446502-11-9)

Enasidenib is a oral potent, selective, reversible inhibitor of mutant IDH2. Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).

Not Intended for Therapeutic Use. For research use only.

CAS: 1446502-11-9 Category

Enasidenib (1446502-11-9) Description:

Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer . The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer.

Enasidenib is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, enasidenib specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG.

Enasidenib (1446502-11-9) Specifications:

Product Name Enasidenib (AG-221)
Synonyms AG-221; AG 221; AG221; CC-90007; CC 90007; CC90007; Enasidenib
Chemical Names 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1446502-11-9
Molecular Formula C19H17F6N7O
Molecular Weight 473.38
Monoisotopic Mass 473.14 g/mol
MDL number N/A
InChIKey DYLUUSLLRIQKOE-UHFFFAOYSA-N
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)
SMILES CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1
Form Powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application Enasidenib is a first-in-class oral selective inhibitor of mutant IDH2 enzymes (isocitrate dehydrogenase 2), for the treatment of adults with relapsed or refractory IDH2-mutated acute myeloid leukemia.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Fathi AT, DiNardo CD, Kline I, Kenvin L, Gupta I, Attar EC, Stein EM, de Botton S; AG221-C-001 Study Investigators. Differentiation Syndrome Associated With Enasidenib, a Selective Inhibitor of Mutant Isocitrate Dehydrogenase 2: Analysis of a Phase 1/2 Study. JAMA Oncol. 2018 Jan 18. doi: 10.1001/jamaoncol.2017.4695. [Epub ahead of print] PubMed PMID: 29346478.
  • 2: Patel SA. Enasidenib-Induced Differentiation Syndrome in IDH2-Mutant Acute Myeloid Leukemia. JAMA Oncol. 2018 Jan 18. doi: 10.1001/jamaoncol.2017.4724. [Epub ahead of print] PubMed PMID: 29346477.
  • 3: Tong Z, Atsriku C, Yerramilli U, Wang X, Li Y, Reyes J, Fan B, Yang H, Hoffmann M, Surapaneni S. Absorption, distribution, metabolism and excretion of an isocitrate dehydrogenase-2 inhibitor enasidenib in rats and humans. Xenobiotica. 2018 Jan 22:1-11. doi: 10.1080/00498254.2018.1425511. [Epub ahead of print] PubMed PMID: 29320949.
  • 4: Perl AE. The role of targeted therapy in the management of patients with AML. Blood Adv. 2017 Nov 14;1(24):2281-2294. doi: 10.1182/bloodadvances.2017009829. eCollection 2017 Nov 14. Review. PubMed PMID: 29296877; PubMed Central PMCID: PMC5737125.
  • 5: Montalban-Bravo G, Garcia-Manero G, Jabbour E. Therapeutic choices after hypomethylating agent resistance for myelodysplastic syndromes. Curr Opin Hematol. 2018 Mar;25(2):146-153. doi: 10.1097/MOH.0000000000000400. PubMed PMID: 29266015.

1 review for Enasidenib (1446502-11-9)

  1. Cofttek

    Never had such good experience before,The Enasidenib (1446502-11-9) is high purity,also customer service is pretty nice !gotta try!!

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