ICI 182,780

Name: ICI 182,780
Brand: Tocris Bioscience
SKU: 1047
Rating: 5 (1 reviews)

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

(1)

Citations (1089)

COA / SDS

Estrogen receptor antagonist

Key Product Details

Description:	Estrogen receptor antagonist
Alternative Names:	Fulvestrant
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)
Molecular Weight:	606.77

View Full Technical Details for ICI 182,780

Technical Data
Citations / Reviews (1)

Biological Activity for ICI 182,780

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.

Compound Libraries for ICI 182,780

ICI 182,780 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for ICI 182,780

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for ICI 182,780

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

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 will 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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References for ICI 182,780

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