ICI 182,780 is a high affinity estrogen receptor antagonist (IC₅₀ = 0.29 nM), devoid of any partial agonism both in vitro and in vivo. ICI 182,780 is a high affinity agonist at the membrane estrogen receptor GPER. ICI 182,780 inhibits MCF-7 human breast cancer cell growth in vitro and shows antitumor activity in mice models. ICI 182,780 penetrates the blood-brain-barrier and has neuronal functional effects in vivo.

Product Specifications

Molecular Weight

606.77

Formula

C₃₂H₄₇F₅O₃S

Storage

Store at RT

Purity

≥98% (HPLC)

Chemical Name

7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	60.68	100
	Ethanol	30.34	50

Preparing Stock Solutions for ICI 182,780

The following data is based on the product molecular weight 606.77

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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	3.30 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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Background References

References are publications that support the biological activity of the product.

Alfinito ICI 182,780 penetrates brain and hypothalamic tissue and has functional effects in the brain after systemic dosing. Endocrinology 2008 PMID: 18599545
Wakeling A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 PMID: 1855205
Howell ICI 182,780 (Faslodex^TM): Development of a novel, "pure" antiestrogen. Cancer 2000 PMID: 10951345
Thomas Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 2005 PMID: 15539556
de Cupis Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting OE and IGF-I induced proliferation of human breast cancer-derived cells. Br.J.Pharmacol. 1995 PMID: 8581274

ICI 182,780

Tocris Bioscience, part of Bio-Techne | Catalog # 1047

Key Product Details

Description

Alternative Names

View all Estrogen and Related Receptor Antagonists »

Product Description