Toremifene Citrate,89778-27-8

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YZ剂描述：

产品名称：Toremifene Citrate

产品别名：枸橼酸托瑞米芬

英文别名：FC 1157a;NK 622

靶点：Estrogen receptor

CAS：89778-27-8

纯度：>98%

外观：白色或类白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Toremifene Citrate (Fareston, Acapodene) is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species.

溶解性：DMSO ：93 mg/mL (155.5 mM)

体外研究：

Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells. Toremifene causes growth inhibition of estrogen-sensitive breast cancer cells by inducing some cells to undergo apoptosis and by inhibiting other cells from entering mitosis. Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation. Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma.

体内研究：Toremifene, at the highest tested dose, increases the incidence of hepatocellular carcinomas in the DEN-initiated groups to a level one-third that observed with Tamoxifen administration to DEN-initiated rats. Toremifene increases the incidence of hypernephromas in previously DEN-initiated rats. Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats.

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