Ospemifene
(Synonyms: 奥培米芬; FC-1271a) 目录号 : GC11996A selective estrogen receptor modulator
Cas No.:128607-22-7
Sample solution is provided at 25 µL, 10mM.
Ospemifene is a selective estrogen for the prevention of postmenopausal osteoporosis with IC50 values of 827nM and 1633nM for ERα and ERβ, respectively. target: ERα and ERβIC50:827 and 1633 nm for ERα and -β, respectively[1] IN vitro: The estrogen-dependent MCF-7 human breast cancer cells were used as a model for studies on the effects of Ospemifene on breast cancer cells. The addition of the compound at concentrations of 0.1 nm to 10 μm did not cause a significant increase in MCF-7 cell growth in vitro when studied by measuring ATP or 3-[4,5-dimethylthiazol-2-yl]2,5-diphenyltetrazolium bromide levels, cell numbers, and rate of [3H]thymidine incorporation during a 7-day culture period. On the other hand, the compound did not inhibit the growth stimulation caused by 1 nm estradiol, except at a concentration 10 mm by only 30%. Similar results were obtained with ZR 75–1 cells, another estrogen-dependent human breast cancer cell line. The cytotoxicity of FC1271a at high concentrations was therefore markedly lower than that for TAM, TOR, or RAL.[1]In ER+ MCF-7 cells, TOR VI and FC-1271a exhibited anti-estrogenic activity. The anti-estrogenic effects of these compounds were less potent as anti-estrogens when compared with TOR and RAL.[2]"In vivo: In the DMBA rat mammary carcinoma model, Ospemifene showed a clear antitumor effect that seemed to be caused primarily by a decrease in the appearance of new tumors but also by a retardation of tumor progression without stimulating the growth of human breast cancer cells.[1]Tumor growth was shown to be inhibited at these doses, indicating anti-estrogenic activity at all doses including 50 and 100 mg/kg Ospemifene. By the end of treatment, MCF-7 tumors in Ospemifene treated mice were statistically smaller compared with control tumors.[2]
References:
[1]. Qiang Qv.et al.Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology.Feb;141(2):809-20. 25. (2000).
[2]. Tracy L. Taras et al.In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. The Journal of Steroid Biochemistry and Molecular Biology 77(4-5):271-9,(2001).
Cas No. | 128607-22-7 | SDF | |
别名 | 奥培米芬; FC-1271a | ||
化学名 | 2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]ethanol | ||
Canonical SMILES | C1=CC=C(C=C1)C(=C(C2=CC=CC=C2)C3=CC=C(C=C3)OCCO)CCCl | ||
分子式 | C24H23ClO2 | 分子量 | 378.89 |
溶解度 | ≥ 15.4mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6393 mL | 13.1964 mL | 26.3929 mL |
5 mM | 0.5279 mL | 2.6393 mL | 5.2786 mL |
10 mM | 0.2639 mL | 1.3196 mL | 2.6393 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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