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Category: Nuclear ReceptorsarrowEstrogen and Related Receptors
Cat.No. Product Name
1047 ICI 182,780
Price and Availability

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ICI 182,780

Other Information:

Sold with the permission of AstraZeneca UK Ltd.

No more than 100 mg per customer per year to be sold
Chemical Name: 7a,17b-[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 ligand at the membrane estrogen receptor GPR30.

Technical Data:

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M.Wt: 606.77
Formula: C32H47F5O3S
Storage: Store at RT
Solubility: Soluble to 50 mM in Ethanol and to 100 mM in DMSO
Purity: >99%
CAS No: [129453-61-8]

Resources:

  • Certificate of Analysis / MSDS:

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    References:

    Wakeling et al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867. 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.  Howell et al (2000) ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89 817. Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinol. 146 624.
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    Keywords: ICI 182,780, Estrogen & Related Receptors, Estrogen Receptor Antagonist, ICI182,780, Tocris Bioscience

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    Estrogen Receptors
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