I4409

Fulvestrant

>98% (HPLC)

• Synonyme(s) : (7a,17b)-7-[9-[(4,4,5,5,5pentafluoropentyl)Sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol, Faslodex, ICI 182,780, ZD 182780, ZD 9238, ZM 182780
• Formule empirique (notation de Hill): C₃₂H₄₇F₅O₃S
• Numéro CAS: 129453-61-8
• Poids moléculaire : 606.77
• Numéro MDL: MFCD00903953
• Code UNSPSC : 51111800
• ID de substance PubChem : 329815373
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: >98% (HPLC)
• Forme: powder
• Solubilité: DMSO: >5 mg/mL
• Auteur: AstraZeneca
• Température de stockage: 2-8°C
• Chaîne SMILES: [H][C@]12CC[C@]3(C)[C@@H](O)CC[C@@]3([H])[C@]1([H])[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)Cc4cc(O)ccc24
• 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
• Clé InChI: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• Informations sur le gène: human ... ESR1(2099) , ESR2(2100)

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

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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.

Informations sur la sécurité

• Mentions de danger: H413
• Conseils de prudence: P273
• Classification des risques: Aquatic Chronic 4
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Équipement de protection individuelle: Eyeshields, Gloves, type N95 (US)