E-2121 Enasidenib, Free Base, >99%

Solubility: DMSO.

ENS-101

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• Enasidenib, also known as AG221, is a potent and selective IDH2 mutant enzyme inhibitor.  It caused a significant decrease in R(-)-2-hydroxyglutarate in marrow, plasma, and urine and showed a dose-dependent survival benefit in a primary human AML xenograft model carrying the IDH2 R140Q mutation.  Wang F., et al. "AG-221 Offers a Survival Advantage In a Primary Human IDH2 Mutant AML Xenograft Model." Blood 122: Abstract 240 (2013).
• Enasidenib is an orally available selective potent inhibitor of the mutant IDH2 enzyme.  It inhibited 2HG production by the IDH2^R140Q homodimer (IC₅₀ = 100 nM), the IDH2^R140Q/WT heterodimer (IC₅₀ = 30 nM), and the IDH2^R172K/WT heterodimer (IC₅₀ = 10 nM), and inhibited the canonical forward (oxidative) reaction in the IDH2^WT homodimer (IC₅₀ = 1.8 μM).  It inhibited 2HG production and promoted cellular differentiation in primary human IDH2 mutation–positive acute myeloid leukemia (AML) cells ex vivo and in xenograft mouse models.  It also provided significant survival benefit in an aggressive IDH2^R140Q-mutant AML xenograft mouse model.  Yen K., et al. "AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations." Cancer Discov. 7: 478-493 (2017).
• Differentiation appears to be the main mechanism of enasidenib efficacy in relapsed/refractory AML patients.  Amatangelo M.D., et al. "Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response." Blood 130: 732-741 (2017).
• Related CAS numbers:  1650550-25-6 for the methanesulfonate salt.
• Enasidenib is the active ingredient in the drug product sold under the trade name Idhifa®.  This drug is currently approved in a least one country for treatment of adult patients with relapsed or refractory acute myeloid leukemia, advanced or metastatic breast cancer and other conditions.  NOTE:  THE ENASIDENIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT IDHIFA®, AND IS NOT FOR HUMAN USE.
  
  
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.