Network Version
Fulvestrant Data Sheet
| Product Name: | Fulvestrant |
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|---|---|---|
| CAS No.: | 129453-61-8 | |
| Cat. No.: | HY-13636 | |
| MWt: | 606.77 | |
| Formula: | C32H47F5O3S | |
| Purity : | >98% | |
| Solubility: | DMSO : 250 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer Inflammation/Immunology | |
| Biological Activity: | ||
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Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
IC50 & Target:IC50: 9.4 nM (Estrogen Receptor)[1]
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[1]. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER[3]. 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[4].
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.[1]. 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[3]. Fulvestrant exhibits tumor growth inhibition (TGI) on day 40 of 88%[4]. |
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