Enasidenib -Biokitchen

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Enasidenib

Time：2016-10-31

CAS#: 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.

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

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

THEORETICAL ANALYSIS

Name: Enasidenib (AG-221)
CAS#: 1446502-11-9
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

TECHNICAL DATA

Appearance:

Solid powder

Purity:

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

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).

REFERENCES

1: Caino MC, Altieri DC. Molecular Pathways: Mitochondrial Reprogramming in Tumor Progression and Therapy. Clin Cancer Res. 2016 Feb 1;22(3):540-5. doi: 10.1158/1078-0432.CCR-15-0460. Epub 2015 Dec 9. PubMed PMID: 26660517; PubMed Central PMCID: PMC4738153.

2: Stein EM. IDH2 inhibition in AML: Finally progress? Best Pract Res Clin Haematol. 2015 Jun-Sep;28(2-3):112-5. doi: 10.1016/j.beha.2015.10.016. Epub 2015 Oct 19. Review. PubMed PMID: 26590767.

3: Rowe JM. Reasons for optimism in the therapy of acute leukemia. Best Pract Res Clin Haematol. 2015 Jun-Sep;28(2-3):69-72. doi: 10.1016/j.beha.2015.10.002. Epub 2015 Oct 22. Review. PubMed PMID: 26590761.

4: Stein EM. Molecular Pathways: IDH2 Mutations-Co-opting Cellular Metabolism for Malignant Transformation. Clin Cancer Res. 2016 Jan 1;22(1):16-9. doi: 10.1158/1078-0432.CCR-15-0362. Epub 2015 Nov 9. PubMed PMID: 26553750.

5: Kiyoi H. Overview: A New Era of Cancer Genome in Myeloid Malignancies. Oncology. 2015;89 Suppl 1:1-3. doi: 10.1159/000431054. Epub 2015 Nov 10. Review. PubMed PMID: 26551625.

6: Tomita A. [Progress in molecularly targeted therapies for acute myeloid leukemia]. Rinsho Ketsueki. 2015 Feb;56(2):130-8. doi: 10.11406/rinketsu.56.130. Japanese. PubMed PMID: 25765792.

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