| 货号 | 17204-500ug |
| 描述 | 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. α-hydroxy Tamoxifen is a reactive metabolite of tamoxifen that is formed by the action of cytochrome P450 3A4 in human liver.1,2 It can be further converted into genotoxic DNA adducts though a mechanism involving reversible O-sulfonation of the hydroxyl moiety, which in rats has been linked with hepatocarcinoma.1,3,4,5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Boocock, D.J.,Maggs, J.L.,White, I.N.H., et al. α-Hydroxytamoxifen, a genotoxic metabolite of tamoxifen in the rat: Identification and quantification in vivo and in vitro. Carcinogenesis 20(1), 153-160 (1999). 2.Mugundu, G.M.,Sallans, L.,Guo, Y., et al. Assessment of the impact of CYP3A polymorphisms on the formation of α-hydroxytamoxifen and N-desmethyltamoxifen in human liver microsomes. Drug Metabolism and Disposition 40(2), 389-396 (2012). 3.White, I.N.H.,Carthew, P.,Davies, R., et al. Short-term dosing of α-hydroxytamoxifen results in DNA damage but does not lead to liver tumours in female Wistar/Han rats. Carcinogenesis 22(4), 553-557 (2001). 4.Yadollahi-Farsani, M.,Davies, D.S., and Boobis, A.R. The mutational signature of α-hydroxytamoxifen at Hprt locus in Chinese hamster cells. Carcinogenesis 23(11), 1947-1952 (2002). 5.Shibutani, S.,Dasaradhi, L.,Terashima, I., et al. α-Hydroxytamoxifen is a substrate of hydroxysteroid (alcohol) sulfotransferase, resulting in tamoxifen DNA adducts. Cancer Research 58(4), 647-653 (1998). 6.Kim, S.Y.,Laxmi, Y.R.S.,Suzuki, N., et al. Formation of tamoxifen-DNA adducts via O-sulfonation, not O-acetylation, of α-hydroxytamoxifen in rat and human livers. Drug Metabolism and Disposition 33(11), 1673-1678 (2005). | |
| 运输条件 | Wet ice 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 | 97151-02-5 |
| 稳定性 | ≥ 2 years |
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