枸橼酸他莫昔芬
Product Name:Tamoxifen Citrate(Nolvadex )
Synonyms:1-p-beta-dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene citrate;(z)-2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethylethanamine,citrate(1:;(z)-2-(para-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethylethylaminecitrate(;2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethyl-ethanamin(z)-ethanamin2-hydrox;ici46,474;kessar;noltam;tamofen
CAS:54965-24-1
MF:C32H37NO8
MW:563.64
EINECS:259-415-2
MP:140-144 °c
Storage Temp. :2-8°C
Water Solubility:slightly soluble
Chemical Properties:white to off-white powder
Biological Activity:Estrogen receptor antagonist/partial agonist. Selective and potent inhibitor of mammalian sterol isomerase. Neuroprotective in female rats in vivo . Also high affinity agonist at the membrane estrogen receptor GPR30.
Uses:For the treatment of advanced and recurrent breast cancer and ovarian cancer, etc.
Clinical Application:
1). Treatment of breast cancer.
2). Prevention of breast cancer.
3). Anti-tumor and anti-multidrug resistance.
By reducing membrane negotiability and enhancing rigidity of inter-cell binding site, Tamoxifen citrate can reduce concentration and activity of cancer metastasis promoter and various activating enzymes, so as to inhibit or hinder growth and metastasis of cancer cell. In addition, it can promote cells surrounding tumor focus to secrete a negative growth factor - transforming growth factor TGF- G, inhibiting multiply indefinitely of cancer cells; inhibiting oxidative damage of DNA bases which is caused by hydrogen peroxide generated from human neutrophils. So except for breast cancer, it is good for treatment and prevention of other malignant neoplasms, and is used for treatment of brain tumors, liver cancer, prostate cancer, etc. In addition, Tamoxifen citrate can reduce release effect of membrane P170 glycoprotein through reducing membrane negotiability, improving intracellular effective concentration of cytotoxic drug and reducing drug resistance 4).Heart protection.
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