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Ospemifene Sale

(Synonyms: 奥培米芬; FC-1271a) 目录号 : GC11996

A selective estrogen receptor modulator

Ospemifene Chemical Structure

Cas No.:128607-22-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥385.00
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5mg
¥225.00
现货
10mg
¥450.00
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50mg
¥595.00
现货
100mg
¥700.00
现货
200mg
¥1,050.00
现货

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产品描述

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).

Chemical Properties

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
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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。
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。

溶解性数据

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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
378.89
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