82413-23-8

White Solid

A metabolite of Tamoxifen (T006000).

4’-hydroxy Tamoxifen is one of five main phase I metabolites of tamoxifen , a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium. 4’-hydroxy Tamoxifen is a product of cytochrome P450 (CYP)2D6 and CYP2B6 activity. With the addition of a hydroxyl group, 4’-hydroxy tamoxifen has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. At 10-100 μM, 4’-hydroxy tamoxifen is cytotoxic, in a non-apoptotic manner, to HEC-1B and HEC-1A human endometrial adenocarcinoma cell lines.

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[3] H SEEGER. Inhibition of human breast cancer cell proliferation with estradiol metabolites is as effective as with tamoxifen.[J]. Hormone and Metabolic Research, 2004, 36 5: 277-280. DOI: 10.1055/s-2004-814480
[4] MARIA E CUEVAS  Tracey E L. In vitro cytotoxicity of 4’-OH-tamoxifen and estradiol in human endometrial adenocarcinoma cells HEC-1A and HEC-1B.[J]. Oncology reports, 2015, 33 1: 464-470. DOI: 10.3892/or.2014.3565
[5] GIORGIA URBINATI. Therapeutic potential of new 4-hydroxy-tamoxifen-loaded pH-gradient liposomes in a multiple myeloma experimental model.[J]. Pharmaceutical Research, 2010, 27 2: 327-339. DOI: 10.1007/s11095-009-0023-z