Enasidenib (AG-221)
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MedKoo CAT#: 206438

CAS#: 1446502-11-9 (free base)

Description: Enasidenib, also 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.


Price and Availability

Size Price Shipping out time Quantity
25mg USD 90 Same day
50mg USD 150 Same day
100mg USD 250 Same day
200mg USD 450 Same day
500mg USD 950 Same day
1g USD 1450 Same day
2g USD 2450 Same day
5g USD 4650 Same day
10g USD 8650 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

Enasidenib, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206438
Name: Enasidenib (AG-221)
CAS#: 1446502-11-9 (free base)
Chemical Formula: C19H17F6N7O
Exact Mass: 473.13988
Molecular Weight: 473.38
Elemental Analysis: C, 48.21; H, 3.62; F, 24.08; N, 20.71; O, 3.38


Related CAS #: 1650550-25-6 (mesylate)   1446502-11-9 (free base)  

Synonym: AG-221; AG 221; AG221; CC-90007; CC 90007; CC90007; Enasidenib; Idhifa

IUPAC/Chemical Name: 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

InChi Key: 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 Code: CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Dittakavi S, Hallur G, Purra BR, Kiran V, Zakkula A, Mullangi R. Validated LC-MS/MS Method for Simultaneous Quantitation of Enasidenib and its Active Metabolite, AGI-16903 in Small Volume Mice Plasma: Application to a Pharmacokinetic Study. Drug Res (Stuttg). 2019 Oct 25. doi: 10.1055/a-1024-3623. [Epub ahead of print] PubMed PMID: 31652462.

2: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548492/ PubMed PMID: 31643811.

3: Reed DR, Elsarrag RZ, Morris AL, Keng MK. Enasidenib in acute myeloid leukemia: clinical development and perspectives on treatment. Cancer Manag Res. 2019 Aug 30;11:8073-8080. doi: 10.2147/CMAR.S162784. eCollection 2019. PubMed PMID: 31564968; PubMed Central PMCID: PMC6724422.

4: Del Principe MI, Paterno G, Palmieri R, Maurillo L, Buccisano F, Venditti A. An evaluation of enasidenib for the treatment of acute myeloid leukemia. Expert Opin Pharmacother. 2019 Nov;20(16):1935-1942. doi: 10.1080/14656566.2019.1654456. Epub 2019 Aug 27. PubMed PMID: 31454277.

5: Zakkula A, Dittakavi S, Maniyar MM, Syed N, Sulochana SP, Zainuddin M, Mullangi R. Validated HPLC method for simultaneous quantification of mutant IDH1/2 inhibitors (enasidenib, ivosidenib and vorasidenib) in mouse plasma: Application to a pharmacokinetic study. Biomed Chromatogr. 2019 Nov;33(11):e4658. doi: 10.1002/bmc.4658. Epub 2019 Sep 2. PubMed PMID: 31325170.

6: Galkin M, Jonas BA. Enasidenib in the treatment of relapsed/refractory acute myeloid leukemia: an evidence-based review of its place in therapy. Core Evid. 2019 Apr 26;14:3-17. doi: 10.2147/CE.S172912. eCollection 2019. PubMed PMID: 31118877; PubMed Central PMCID: PMC6503332.

7: Pollyea DA, Tallman MS, de Botton S, Kantarjian HM, Collins R, Stein AS, Frattini MG, Xu Q, Tosolini A, See WL, MacBeth KJ, Agresta SV, Attar EC, DiNardo CD, Stein EM. Enasidenib, an inhibitor of mutant IDH2 proteins, induces durable remissions in older patients with newly diagnosed acute myeloid leukemia. Leukemia. 2019 Nov;33(11):2575-2584. doi: 10.1038/s41375-019-0472-2. Epub 2019 Apr 9. PubMed PMID: 30967620.

8: Li Y, Connarn JN, Chen J, Tong Z, Palmisano M, Zhou S. Modeling and simulation of the endogenous CYP3A induction marker 4β-hydroxycholesterol during enasidenib treatment. Clin Pharmacol. 2019 Feb 15;11:39-50. doi: 10.2147/CPAA.S192687. eCollection 2019. PubMed PMID: 30858735; PubMed Central PMCID: PMC6385784.

9: Myers RA, Wirth S, Williams S, Kiel PJ. Enasidenib: An Oral IDH2 Inhibitor for the Treatment of Acute Myeloid Leukemia. J Adv Pract Oncol. 2018 May-Jun;9(4):435-440. Epub 2018 May 1. Review. PubMed PMID: 30719396; PubMed Central PMCID: PMC6347084.

10: Dittakavi S, Jat RK, Mullangi R. Quantitative analysis of enasidenib in dried blood spots of mouse blood using an increased-sensitivity LC-MS/MS method: Application to a pharmacokinetic study. Biomed Chromatogr. 2019 Jun;33(6):e4491. doi: 10.1002/bmc.4491. Epub 2019 Feb 7. PubMed PMID: 30663096.

11: Stein EM, DiNardo CD, Fathi AT, Pollyea DA, Stone RM, Altman JK, Roboz GJ, Patel MR, Collins R, Flinn IW, Sekeres MA, Stein AS, Kantarjian HM, Levine RL, Vyas P, MacBeth KJ, Tosolini A, VanOostendorp J, Xu Q, Gupta I, Lila T, Risueno A, Yen KE, Wu B, Attar EC, Tallman MS, de Botton S. Molecular remission and response patterns in patients with mutant-IDH2 acute myeloid leukemia treated with enasidenib. Blood. 2019 Feb 14;133(7):676-687. doi: 10.1182/blood-2018-08-869008. Epub 2018 Dec 3. PubMed PMID: 30510081; PubMed Central PMCID: PMC6384189.

12: Tong Z, Yerramilli U, Yao S, Young JD, Hoffmann M, Surapaneni S. In vitro inhibition of human nucleoside transporters and uptake of azacitidine by an isocitrate dehydrogenase-2 inhibitor enasidenib and its metabolite AGI-16903. Xenobiotica. 2019 Oct;49(10):1229-1236. doi: 10.1080/00498254.2018.1539783. Epub 2018 Nov 29. PubMed PMID: 30394160.

13: Li Y, Liu L, Gomez D, Chen J, Tong Z, Palmisano M, Zhou S. Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects. Pharmacol Res Perspect. 2018 Oct 23;6(6):e00436. doi: 10.1002/prp2.436. eCollection 2018 Dec. PubMed PMID: 30386625; PubMed Central PMCID: PMC6199364.

14: Dogra R, Bhatia R, Shankar R, Bansal P, Rawal RK. Enasidenib: First Mutant IDH2 Inhibitor for the Treatment of Refractory and Relapsed Acute Myeloid Leukemia. Anticancer Agents Med Chem. 2018;18(14):1936-1951. doi: 10.2174/1871520618666181025091128. Review. PubMed PMID: 30360730.

15: Galeotti J, Coombs CC. Enasidenib-induced eosinophilic differentiation in a patient with acute myeloid leukaemia with IDH2 and U2AF1 mutations. Br J Haematol. 2019 Feb;184(4):496. doi: 10.1111/bjh.15609. Epub 2018 Oct 18. PubMed PMID: 30334576.

16: Krämer A, Bochtler T. Enasidenib. Recent Results Cancer Res. 2018;212:187-197. doi: 10.1007/978-3-319-91439-8_9. PubMed PMID: 30069631.

17: Abou Dalle I, DiNardo CD. The role of enasidenib in the treatment of mutant IDH2 acute myeloid leukemia. Ther Adv Hematol. 2018 Jul;9(7):163-173. doi: 10.1177/2040620718777467. Epub 2018 Jun 1. Review. PubMed PMID: 30013764; PubMed Central PMCID: PMC6041864.

18: Quek L, David MD, Kennedy A, Metzner M, Amatangelo M, Shih A, Stoilova B, Quivoron C, Heiblig M, Willekens C, Saada V, Alsafadi S, Vijayabaskar MS, Peniket A, Bernard OA, Agresta S, Yen K, MacBeth K, Stein E, Vassiliou GS, Levine R, De Botton S, Thakurta A, Penard-Lacronique V, Vyas P. Clonal heterogeneity of acute myeloid leukemia treated with the IDH2 inhibitor enasidenib. Nat Med. 2018 Aug;24(8):1167-1177. doi: 10.1038/s41591-018-0115-6. Epub 2018 Jul 16. PubMed PMID: 30013198.

19: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500925/ PubMed PMID: 29999984.

20: Roboz GJ. Enasidenib for relapsed/refractory acute myeloid leukemia with IDH2 mutations: optimizing the patient experience. Clin Adv Hematol Oncol. 2018 May;16(5):322-325. PubMed PMID: 29851927.