13021  2-Methoxyestradiol

Panzem; NSC 659853; 2-ME2; 2-Hydroxyestradiol 2-methyl ether (CAS 362-07-2)




For active pharmaceutical ingredients (APIs) related to 2-Methoxyestradiol, see Cayman Pharma

2-methoxy Estradiol (2-ME2) is a natural metabolite formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol. Administration of 2-hydroxy estradiol (2-HE2) to rats results in formation and clearance of 2-ME2 with t½ values of 7.9 and 24.9 minutes, respectively.1 2-ME2 exhibits no affinity for estrogen receptors. 2-ME2 has achieved considerable attention as an anti-cancer agent acting as an angiogenesis inhibitor via the HIF-1a pathway.2,3,4 The levels of COMT and 2-ME2 are significantly lower in women with severe pre-eclampsia.5
1  Zacharia, L.C., Piché, C.A., Fielding, R.M., et al. 2-hydroxyestradiol is a prodrug of 2-methoxyestradiol. J Pharmacol Exp Ther 309(3) 1093-1097 (2004).
2  Mooberry, S.L. New insights into 2-methoxyestradiol, a promising antiangiogenic and antitumor agent. Curr Opin Oncol 15 425-430 (2003).
3  Mooberry, S.L. Mechanism of action of 2-methoxyestradiol: New developments. Drug Resist Updat 6 355-361 (2003).
4  Becker, C.M., Rohwer, N., Funakoshi, T., et al. 2-methoxyestradiol inhibits hypoxia-inducible factor-1a and suppressess growth of lesions in a mouse model of endometriosis. Am J Pathol 172(2) 534-544 (2008).
5  Kanasaki, K., Palmsten, K., Sugimoto, H., et al. Deficiency in catechol-O-methyltransferase and 2-methoxyoestradiol is associated with pre-eclampsia. Nature 453 1117-1123 (2008).

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Pricing Information

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Size Price Quantity
5 mg €28.00
10 mg €53.00
25 mg €125.00
50 mg €221.00
Pricing updated 2010-08-01.
Prices are subject to change without notice.