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.
Technical Data
| M. Wt | 606.77 |
| Formula | C32H47F5O3S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 129453-61-8 |
| PubChem ID | 17756771 |
| InChI Key | VWUXBMIQPBEWFH-LQKBAPIOSA-N |
| Smiles | OC1=CC=C2C(C[C@@H](CCCCCCCCCS(CCCC(F)(C(F)(F)F)F)=O)C3([H])[C@@]([H])2CC[C@@]4(C)[C@@](CC[C@@H]4O)3[H])=C1 |
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
References
References are publications that support the products' biological activity.
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
Wakeling et al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867 PMID: 1855205
Keywords: ICI 182,780, supplier, High, affinity, GPR30, agonist, Estrogen, receptors, antagonists, ER, ERR, ICI182780, AstraZeneca, GPER, Estrogen, and, Related, Receptors, Estrogen, (GPER), Receptors, Estrogen, and, Related, Receptors, Tocris Bioscience
