货号 | 11629-500mg |
描述 | Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.1 TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.2 TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.3 In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.4 |
别名 | ICI 46474;Istubal;Kessar;Noltam;Nolvadex;TMX;Valodex;Zemide; |
供应商 | Cayman |
应用文献 | |
1.Clarke, M.,Collins, R.,Davies, C., et al. Tamoxifen for early breast cancer: An overview of the randomised trials. Lancet 351, 1451-1467 (1998). 2.Hall, J.M.,Couse, J.F., and Korach, K.S. The multifaceted mechanisms of estradiol and estrogen receptor signaling. The Journal of Biological Chemisty 276(40), 36869-26872 (2001). 3.Singh, M.S.,Francis, P.A., and Michael, M. Tamoxifen, cytochrome P450 genes and breast cancer clinical outcomes. Breast 20, 111-118 (2011). 4.de Medina, P.,Paillasse, M.R.,Ségala, G., et al. Importance of cholesterol and oxysterols metabolism in the pharmacology of tamoxifen and other AEBS ligands. Chemistry and Physics of Lipids 164, 432-437 (2011). | |
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 | 563.6 |
分子式 | C26H29NO • C6H8O7 |
CAS号 | 54965-24-1 |
稳定性 | ≥ 2 years |
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