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• {SNA} Antibiotics A to Z, Antibiotics G-M, Antibiotics by Application, Antineoplastic and Immunosuppressive Antibiotics, Antitumor Agents, Approved Therapeutics/Drug Candidates, AstraZeneca, Bioactive Small Molecule Alphabetical Index, Cytokines, Growth Factors and Hormones, Estrogen Modulators, Fluorination Ready Pharma-Developed Compounds, Gene Regulation, H, Hormones,
• {SNA} Additional Drugs, Analytical Standards, Antibiotics A to Z, Antibiotics G-M, Antibiotics by Application, Antineoplastic and Immunosuppressive Antibiotics, Pharmaceuticals, Illicit Drugs & Alcohol, 分析/色谱, 抗生素, 生化试剂
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产品应用

• Afimoxifene (4-hydroxytamoxifen) is a selective estrogen receptor modulator which is the active metabolite of tamoxifen. Afimoxifene is a transdermal gel formulation and is being developed by Ascend Therapeutics, Inc. under the trademark TamoGel. Afimoxifene has completed a phase II clinical trial for the treatment of cyclical mastalgia. A study in France on 55 women showed that rubbing afimoxifene on the skin was as good as tamoxifen tablets at slowing breast cancer growth. A US trial will compare 6 weeks use before breast cancer surgery. Skin application can reduce systemic levels by a factor of nine and this is expected to reduce the unpleasant side-effects of tamoxifen. (source: http://en.wikipedia.org/wiki/Afimoxifene).

相关文献及参考

• Levenson, A., et al.: Cancer Lett., 125, 215 (1998),
• Zhao, C., et al.: J. Steroid Biochem. Mol. Biol., 98, 1 (2006),
• Bellavance, E., et al.: J. Med. Chem., 52, 7488 (2009),
• McCague R, et al., Nonisomerizable analogues of (Z)- and (E)-4-hydroxytamoxifen; Synthesis and endocrinological properties of substituted diphenylbenzocycloheptenes J. Med. Chem. 31 , 1285-1290, (1988) 摘要
• Osborne CK, et al., Acquired tamoxifen resistance: correlation with reduced breast tumor levels of tamoxifen and isomerization of trans-4-hydroxytamoxifen J. Natl. Cancer Inst. 83 , 1477-1482, (1991) 摘要
• Osborne CK, et al., Tamoxifen and the isomers of 4-hydroxytamoxifen in tamoxifen-resistant tumors from breast cancer patients J. Clin. Oncol. 10 , 304-310, (1992) 摘要
• Yu DD, and Forman BM., Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator J. Org. Chem. 68 , 9489-9491, (2003) 摘要
• Zheng Y, et al., Elimination of antiestrogenic effects of active tamoxifen metabolites by glucuronidation Drug Metab. Dispos. 35 , 1942-1948, (2007) 摘要
• Bechard, M., and Dalton, S., Subcellular Localization Of Glycogen Synthase Kinase 3beta Controls Embryonic Stem Cell Self-renewal. Mol. Cell. Biol. 29 , 2092-104, (2009) 摘要
• Bechard, M., et al., Subcellular Localization Of Glycogen Synthase Kinase 3β Controls Embryonic Stem Cell Self-Renewal Mol. Cell. Biol. 29 , 2092-2104, (2009) 摘要
• Lee, G., et al., Response Of Small Intestinal Epithelial Cells To Acute Disruption Of Cell Division Through CDC25 Deletion. Proc. Natl. Acad. Sci. U. S. A. 106 , 4701-6, (2009) 摘要
• Jimenez-Guri, E., et al., Clonal Analysis In Mice Underlines The Importance Of Rhombomeric Boundaries In Cell Movement Restriction During Hindbrain Segmentation. PLoS ONE 5

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