| 货号 | 19519-5mg |
| 描述 | 4’-hydroxy Tamoxifen is one of five main phase I metabolites of tamoxifen (Item No. 13258), 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.1,2,3 With the addition of a hydroxyl group, 4’-hydroxy tamoxifen has been shown to have a higher affinity for estrogen receptors compared to tamoxifen.4 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.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Crewe, H.K.,Notley, L.M.,Wunsch, R.M., et al. Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: Formation of the 4-hydroxy, 4-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metabolism and Disposition 30(8), 869-874 (2002). 2.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). 3.Dahmane, E.,Boccard, J.,Csajka, C., et al. Quantitative monitoring of tamoxifen in human plasma extended to 40 metabolites using liquid-chromatography high-resolution mass spectrometry: New investigation capabilities for clinical pharmacology. Analytical and Bioanalytical Chemistry 406(11), 2627-2640 (2016). 4.Ruenitz, P.C.,Bagley, J.R., and Mokler, C.M. Estrogenic and antiestrogenic activity of monophenolic analogues of tamoxifen, (Z)-2-[p-(1,2-diphenyl-1-butenyl)phenoxy]-N, N-dimethylethylamine. Journal of Medicinal Chemistry 25(9), 1056-1060 (1982). 5.Cuevas, M.E., and Lindeman, T.E. In vitro cytotoxicity of 4-OH-tamoxifen and estradiol in human endometrial adenocarcinoma cells HEC-1A and HEC-1B. Oncology Reports 33(1), 464-470 (2016). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% (may contain up to 10% of the (E) isomer) |
| 计算分子量 | 387.5 |
| 分子式 | C26H29NO2 |
| CAS号 | 82413-23-8 |
| 稳定性 | ≥ 2 years |
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