Toremifene枸橼酸托瑞米芬,89778-27-8

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Toremifene citrate

CAS No. : 89778-27-8

MCE 国际站：Toremifene citrate

产品活性：Toremifene citrate (Z-Toremifene citrate) 是第二代选择性雌激素受体调节剂，对雌激素受体的 IC₅₀ 为 1μM。Toremifene citrate 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC₅₀ 分别为 0.07 µM 和 2.6 µM。

研究领域：Vitamin D Related/Nuclear Receptor  |  Apoptosis

作用靶点：Estrogen Receptor/ERR  |  Apoptosis

In Vitro: Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT with prostate cancer.
The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro.

In Vivo: The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone.

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