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Fulvestrant

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产品价格:电议      采购度:1602      原产地:美洲

发布时间:2021/7/24 4:24:38      所属地区:上海 上海市

简要描述:

Fulvestrant (ICI 182780) 是一种纯抗雌激素,也是一种有效的雌激素受体 (ER) 拮抗剂,IC50 为 nM。Fulvestrant 还是一种 GPR30 的激动剂。Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长,IC50 为 nM。Fulvestrant 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤功效。

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Fulvestrant

CAS No. : 129453-61-8

MCE 站:Fulvestrant

产品活性:Fulvestrant (ICI 182780) 是一种纯抗雌激素,也是一种有效的雌激素受体 (ER) 拮抗剂,IC50 为 9.4 nM。Fulvestrant 还是一种 GPR30 的激动剂。Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长,IC50 为 0.29 nM。Fulvestrant 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤功效。

研究领域:Others  |  Autophagy  |  Apoptosis

作用靶点:Estrogen Receptor/ERR  |  Autophagy  |  Apoptosis

In Vitro: Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with the IC50 of 0.29 nM. The relative binding affinities of Fulvestrant is 0.89. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER. Treatment of MCF-7 cells with 1 ?M ICI 47699 has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression.

In Vivo: When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity. Complete antagonism of Estrogen action is achieved with a dose of 0.5 mg Fulvestrant/kg/day s.c. The effects of Fulvestrant administered p.o. are qualitatively similar but potency is reduced by an order of magnitude compare with s.c. dosing (ED50 0.46 and complete antagonism at 5 mg/kg/day p.o.). The anti-tumor activity of Fulvestrant is first demonstrated in two models of human breast cancer in nude mice. In one of these models, the growth of MCF-7 tumor xenografts is completely blocked for at least 4 weeks following a single injection of Fulvestrant 5 mg. Similar reductions in growth are seen in the Br10 human tumor model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumor growth is delayed to a greater extent than is observed with ICI 47699 treatment. ICI 47699-resistant breast tumors, which grow in nude mice after long-term treatment with ICI 47699, remain ensitive to growth inhibition by Fulvestrant. These are comparable to the tumor growth inhibition (TGI) observed for ICI 47699 and Fulvestrant, which on day 40 are 86 and 88%, respectively.

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更新时间:2024/1/2 10:14:41

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