I4409

Fulvestrant

>98% (HPLC)

• Sinónimos: (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
• Fórmula empírica (notación de Hill): C₃₂H₄₇F₅O₃S
• Número de CAS: 129453-61-8
• Peso molecular: 606.77
• Número MDL: MFCD00903953
• Código UNSPSC: 51111800
• ID de la sustancia en PubChem: 329815373
• NACRES: NA.77

Propiedades

• Análisis: >98% (HPLC)
• formulario: powder
• solubilidad: DMSO: >5 mg/mL
• emisor: AstraZeneca
• temp. de almacenamiento: 2-8°C
• cadena 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
• Clave InChI: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• Información sobre el gen: human ... ESR1(2099) , ESR2(2100)

Descripción

Aplicación

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

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

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.

Información de seguridad

• Frases de peligro: H413
• Consejos de prudencia: P273
• Clasificaciones de peligro: Aquatic Chronic 4
• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Equipo de protección personal: Eyeshields, Gloves, type N95 (US)