Toremifene(Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Toremifene (Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

Toremifene (Z-Toremifene) 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 还可以有效抑制传染性 EBOV ZaireMarburg (MARV)IC50 分别为 0.07 µM 和 2.6 µM。

Toremifene(Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

Toremifene Chemical Structure

CAS No. : 89778-26-7

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Toremifene 的其他形式现货产品:

Toremifene citrate

生物活性

Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].

体外研究
(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[1].
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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

405.96

Formula

C26H28ClNO

CAS 号

89778-26-7

中文名称

托瑞米芬;涛瑞米芬

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Matthew R Smith, Selective Estrogen Receptor Modulators to Prevent Treatment-Related Osteoporosis.Rev Urol. 2005; 7(Suppl 3): S30-S35.

    [2]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.

    [3]. Gauri J Sabnis, Luciana Macedo, Olga Goloubeva, Toremifene – Atamestane; Alone or In Combination: Predictions from the Preclinical Intratumoral Aromatase Model. J Steroid Biochem Mol Biol. 2008 January; 108(1-2): 1-7.

    [4]. Taneja SS, Morton R, Barnette G, Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene. J Clin Oncol. 2013 Feb 10;31(5):523-9.

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