托瑞米芬(Z-托瑞米芬)是一种用于预防骨质疏松症的第二代选择性雌激素受体调节剂(SERM)。
Cas No. | 89778-26-7 |
别名 | 托瑞米芬,Acapodene;Chlortamoxifen;Farestone;GTx 006;Z-Toremifene |
化学名 | (E)-2-(4-(4-chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)-N,N-dimethylethanamine |
Canonical SMILES | CN(CCOC1=CC=C(/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)\CCCl)C=C1)C |
分子式 | C26H28ClNO |
分子量 | 405.96 |
溶解度 | Soluble in DMSO or Water or ethanol |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50 Value: 1±0.3μM. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT in men with prostate cancer [1]. in vitro: 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[2]. 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[2]. Clinical trial: Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene[3]. |