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Tamoxifen citrate is used as an antiestrogen with potent anti-cancer and PKC inhibitory activities. Tamoxifen Citrate functions as an estrogen receptor antagonist in breast tissue. Tamoxifen Citrate is an agonist towards this receptor in tissues of the endometrium. Tamoxifen Citrate inhibits DNA synthesis and transcription by recruiting co-repressors, which stop estrogen from interacting with genes. When combined with PAX2, Tamoxifen Citrate can inhibit the proliferation of ERBB2. It is also a high affinity activator of the GPR30 receptor. Tamoxifen Citrate is an activator of Estrogen Receptor.
Wakeling et al. Non-steroidal anti-estrogens - receptor binding and biological response in rat uterus, rat mammary carcinoma and human breast cancer cells. J.Steroid.Biochem. 1984, 20,(1), 111-20.
Paul et al. Both the immunosuppressant SR31747 and the antioestrogen tamoxifen bind to an emopamil-insensitive site of mammalian Δ8-Δ7 sterol isomerase. J.Pharmacol.Exp.Ther. 1998, 285,(3), 1296-302.
Hazard Statements: H302-H350-H360-H362
Harmful if swallowed. May cause cancer. May damage fertility or the unborn child. May cause harm to breast-fed children.
Precautionary Statements: P263-P260u-P201-P280-P405-P501a
Avoid contact during pregnancy/while nursing. Obtain special instructions before use. Wear protective gloves/protective clothing/eye protection/face protection. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations.