ICI 182,780Cat. No. 1047 |
Price and AvailabilityBy clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.Special ConditionsNo more than 1 g per customer per year to be sold. |
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Chemical Name: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol |
Biological Activity
A high affinity estrogen receptor antagonist (IC50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo. Also high affinity agonist at the membrane estrogen receptor GPR30.Licensing Information
Sold with the permission of AstraZeneca UK Ltd.Certificate of Analysis / Safety Data Sheet
References
Wakeling et al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867. PMID: 1855205.
de Cupis et al (1995) Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting oestradiol and IGF-I induced proliferation of human breast cancer-derived cells. Br.J.Pharmacol. 116 2391. PMID: 8581274.
Howell et al (2000) ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89 817. PMID: 10951345.
Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 146 624. PMID: 15539556.
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Keywords: ICI 182,780, supplier, High, affinity, GPR30, agonist, Estrogen, receptors, antagonists, ER, ERR, ICI182780, AstraZeneca
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