| 货号 | 18642-1mg |
| 描述 | Tamoxifen (Item No. 13258) is a selective estrogen receptor modulator that evokes tissue-dependent effects.1,2,3,4 Tamoxifen N-oxide is a metabolite of tamoxifen that is produced by the action of flavin-containing monooxygenases.5,6 It can be converted back to tamoxifen by cytochrome P450 isoforms and hemoglobin.7,6 Like the parent compound, tamoxifen N-oxide can form DNA adducts.8,9,5 Tamoxifen N-oxide is a weak inhibitor of human hydroxysteroid sulfotransferase 2A1 (Kis = 9.1 and 16.9 µM for the sulfonation of dehydroepiandrosterone and pregnenolone, respectively).10 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Horwitz, K.B., and McGuire, W.L. Nuclear mechanisms of estrogen action. Effects of estradiol and anti-estrogens on estrogen receptors and nuclear receptor processing. The Journal of Biological Chemisty 253(22), 8185-8191 (1978). 2.Clarke, M.,Collins, R.,Davies, C., et al. Tamoxifen for early breast cancer: An overview of the randomised trials. Lancet 351, 1451-1467 (1998). 3.Tonetti, D.A., and Jordan, V.C. Targeted anti-estrogens to treat and prevent diseases in women. Mol. Med. Today 2(5), 218-223 (1996). 4.Jordan, V.C., and Assikis, V.J. Endometrial carcinoma and tamoxifen: Clearing up a controversy. Clinical Cancer Research 1(5), 467-472 (1995). 5.Zhao, L.,Krishnan, S.,Zhang, Y., et al. Differences in metabolitw-mediated toxicity of Tamoxifen in rodents vs. humans elucidated with DNA/microsomes electro-optical arrays and nanoreactors. Chemical Research in Toxicology 22(2), 341-347 (2009). 6.Parte, P., and Kupfer, D. Oxidation of tamoxifen by human flavin-containing monooxygenase (FMO) 1 and FMO3 to tamoxifen-N-oxide and its novel reduction back to tamoxifen by human cytochromes P450 and hemoglobin. Drug Metabolism and Disposition 33(10), 1446-1452 (2005). 7.Gjerde, J.,Gandini, S.,Guerrieri-Gonzaga, A., et al. Tissue distribution of 4-hydroxy-N-desmethyltamoxifen and tamoxifen-N-oxide. Breast Cancer Research and Treatment 134(2), 693-700 (2012). 8.Phillips, D.H.,Hewer, A.,Horton, M.N., et al. N-demethylation accompanies α-hydroxylation in the metabolic activation of tamoxifen in rat liver cells. Carcinogenesis 20(10), 2003-2009 (1999). 9.Shibutani, S.,Suzuki, N.,Laxmi, S.Y.R., et al. Identification of tamoxifen-DNA adducts in monkeys treated with tamoxifen. Cancer Research 63(15), 4402-4406 (2003). 10.Squirewell, E.J.,Qin, X., and Duffel, M.W. Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metabolism and Disposition 42(11), 1843-1850 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 387.5 |
| 分子式 | C26H29NO2 |
| CAS号 | 75504-34-6 |
| 稳定性 | ≥ 2 years |
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