Chemical Name: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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 GPER.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries
ICI 182,780 is also offered as part of the
Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
60.68
100
ethanol
30.34
50
Preparing Stock Solutions
The following data is based on the product molecular weight 606.77. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.65 mL
8.24 mL
16.48 mL
5 mM
0.33 mL
1.65 mL
3.3 mL
10 mM
0.16 mL
0.82 mL
1.65 mL
50 mM
0.03 mL
0.16 mL
0.33 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
de Cupiset 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
Howellet al (2000) ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89 817 PMID: 10951345
Thomaset al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 146 624 PMID: 15539556
Wakelinget al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867 PMID: 1855205