5.31042

Estrogen Receptor Antagonist, ICI 182,780

• Synonym(s): Estrogen Receptor Antagonist, ICI 182,780, GPR30 Agonist, ICI 182,780, ICI 182780, ICI182780
• Empirical Formula (Hill Notation): C₃₂H₄₇F₅O₃S
• CAS Number: 129453-61-8
• Molecular Weight: 606.77
• MDL number: MFCD00903953
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1
• InChI key: VWUXBMIQPBEWFH-WCCTWKNTSA-N

Description

General description

A cell-permeable estradiol derivative that acts as an estrogen antagonist and down-regulates estrogen receptors without affecting estrogen receptor-mediated progesterone receptor expression. Hence, it lacks estrogen agonist activity. Shown to be more effective than tamoxifen in reducing estrogen receptors in breast tumor cells. Suppresses the growth of MCF-7 xenografts in mice for twice as long as tamoxifen and delays tumor growth.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable estradiol derivative that acts as an estrogen antagonist and down-regulates estrogen receptors without affecting estrogen receptor-mediated progesterone receptor expression. Hence, it lacks estrogen agonist activity. Shown to be more effective than tamoxifen in reducing estrogen receptors in breast tumor cells. Suppresses the growth of MCF-7 xenografts in mice for twice as long as tamoxifen and delays tumor growth.



Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable estrogen antagonist. More effective than tamoxifen in reducing estrogen receptors in breast tumor cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ER

Secondary Target
GPR30

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Wakeling, A. E., et al. 1991. Cancer Res.51, 3867.
Dauvois, S., et al. 1993. J. Cell. Sci.106, 1377.
Howell, A., et al. 1995. The Lancet.8941, 29.
Robertson, J.F., et al. 2001. J. Steroid Biochem. Mol Biol.79, 209.

Legal Information

Sold with the permission of AstraZeneca UK. Limited for research purposes only.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Hazard Statements: H413
• Precautionary Statements: P273 - P501
• Hazard Classifications: Aquatic Chronic 4
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3