Sigma-Aldrich Estrogen Receptor Antagoni

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

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: yesPrimary Target
ERSecondary 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.Sold with the permission of AstraZeneca UK. Limited for research purposes only.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, GermanyH413P273 - P501