Pricing updated 2019-02-22. Prices are subject to change without notice.
Tamoxifen (Item No. 13258) is a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. Although it is an antagonist of ER action in breast tissue, it acts as an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues. (E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.1 It exhibits more potent estrogen agonist/antagonist activity than its parent compound and can inhibit MCF-7 and MDA-MB-231 cell proliferation with IC50 values of 27 and 18 µM, respectively.2 (E/Z)-4-hydroxy Tamoxifen has been used to stimulate LC3 lipidation and formation of autophagic vesicles in a superoxide-dependent manner.3
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1. Desta, Z., Ward, B.A., Soukhova, N.V., et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: Prominent roles for CYP3A and CYP2D6 Journal of Pharmacology and Experimental Therapeutics 310(3), 1062-1075 (2004).
2. Seeger, H., Huober, J., Wallwiener, D., et al. Inhibition of human breast cancer cell proliferation with estradiol metabolites is as effective as with tamoxifen Hormone and Metabolic Research 36(5), 277-280 (2004).
Duan, L., Danzer, B., Levenson, V.V., et al. Critical roles for nitric oxide and ERK in the completion of prosurvival autophagy in 4OHTAM-