Tuesday 16 August 2022 - 03:30
In Business 42 Years - Since 1980
PLEASE NOTE: During August 2022 we are doing a comprehensive revision of our customer service workflow. This includes training of current and new personnel. We are expecting that these changes will have only very minimal effects on our overall order processing and shipping activities. However, we do ask any customers who prefer that their shipments go out on Fridays to contact our Customer Service group and let them know about your preferences in advance. Thank you.
Reminder: Genuine LC Laboratories® brand PMA, which we have been manufacturing in the U.S. for more
than 40 years, is available directly from us: Cat No. P-1680 Phorbol 12-Myristate 13-Acetate, >99.5%.
Our PMA is also available from our >50 U.S. and international distributors, and from more than a dozen
major biochemical reagent "resellers" (who sell our PMA under their own brand names and labels)
FREE SHIPPING TO THE U.S. AND 32 OTHER COUNTRIES! [Read more].
E-2121 Enasidenib, Free Base, >99%
Synonyms : [AG221]
Related Terms : [IDHIFA]
- Size
- US $
- €
- £
- ¥
- 5 mg
- 39
- 38
- 32
- 5,200
- In stock
- 10 mg
- 53
- 51
- 43
- 7,000
- In stock
- 25 mg
- 59
- 57
- 48
- 7,800
- In stock
- 50 mg
- 82
- 80
- 67
- 10,900
- In stock
- 100 mg
- 150
- 147
- 124
- 19,900
- In stock
- 200 mg
- 262
- 256
- 216
- 34,800
- In stock
- 500 mg
- 555
- 543
- 458
- 73,600
- In stock
- 1 g
- 976
- 956
- 807
- 129,500
- In stock
- 2 g
- 1,510
- 1,479
- 1,248
- 200,300
- In stock
Note: Our Euro, Pound, and Yen prices are revised regularly to account for currency exchange rate fluctuations.
- M.W. 473.38
- C19H17F6N7O
- [1446502-11-9]
Solubility: DMSO.
- 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 IDH2R140Q homodimer (IC50 = 100 nM), the IDH2R140Q/WT heterodimer (IC50 = 30 nM), and the IDH2R172K/WT heterodimer (IC50 = 10 nM), and inhibited the canonical forward (oxidative) reaction in the IDH2WT 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 IDH2R140Q-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.
