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Fulvestrant

CAS No. : 129453-61-8

MCE 国际站：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：Vitamin D Related/Nuclear Receptor  |  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 μM 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.), Fulvestrant (ICI 182,780) is devoid of uterotropic activity in immature female rats.
Fulvestrant (0.5 mg/kg/day s.c) shows complete antagonism of Estrogen action.
Fulvestrant by po administration (5 mg/kg/day p.o.) is qualitatively similar with s.c..
In two models of human breast cancer in nude mice. In one of these models, Fulvestrant (5 mg) completely blocks the growth of MCF-7 tumor xenografts for at least 4 weeks following a single injection.
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.
Fulvestrant exhibits tumor growth inhibition (TGI) on day 40 of 88%.

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