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I4409 Sigma-Aldrich

Fulvestrant

>98% (HPLC)

Synonym: (7α,17β)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol, Faslodex, ICI 182,780, ZD 182780, ZD 9238, ZM 182780

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Properties

Related Categories Approved Therapeutics/Drug Candidates, AstraZeneca, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
InChI Key   VWUXBMIQPBEWFH-WCCTWKNTSA-N
assay   >98% (HPLC)
form   powder
solubility   DMSO: >5 mg/mL
originator   AstraZeneca
storage temp.   2-8°C

Description

Application

Fulvestrant has been used:
• as an antagonist of estrogen receptor (ERα and ERβ) to reduce hepatocytes proliferation
• as an antagonist of ER for the suppression of estrogen responsive element in human breast cancer MCF-7 cells
• as anti-estrogen in breast cancer cell lines

Packaging

25 mg in glass bottle

Biochem/physiol Actions

Fulvestrant (ICI 182,780) is a selective estrogen receptor down-regulator (SERD). Fulvestrant is a high affinity estrogen receptor antagonist. IC50 = 0.29 nM. Fulvestrant is the first "pure" antiestrogen with no agonistic activity both in vitro and in vivo.

Fulvestrant is a 7α-alkylsulphinyl analog of 17β-oestradiol and is structurally different compared to other selective estrogen receptor (ER) modulators (SERMs). It reduces dimerization and nuclear localization of the estrogen receptor (ER). Fulvestrant lowers the level of ER protein in human breast cancer cells. Fulvestrant is preferred for the treatment of women at their menopause having hormone-sensitive advanced breast cancer.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3
RTECS 
KG7623000

Documents

Certificate of Analysis

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Certificate of Origin

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Milli-Q® Water Purification Solutions
Protocols & Articles
Peer-Reviewed Papers
15

References

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