I4409

Fulvestrant

>98% (HPLC)

• Sinônimo(s): (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
• Fórmula empírica (Notação de Hill): C₃₂H₄₇F₅O₃S
• Número CAS: 129453-61-8
• Peso molecular: 606.77
• Número MDL: MFCD00903953
• Código UNSPSC: 51111800
• ID de substância PubChem: 329815373
• NACRES: NA.77

Propriedades

• Ensaio: >98% (HPLC)
• Formulário: powder
• solubilidade: DMSO: >5 mg/mL
• originador: AstraZeneca
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres 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
• chave InChI: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• Informações sobre genes: human ... ESR1(2099) , ESR2(2100)

Descrição

Aplicação

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

Ações bioquímicas/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.

Fulvestrant is a selective estrogen receptor down-regulator (SERD); high affinity estrogen receptor antagonist.

Características e benefícios

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.

Informações de segurança

• Pictogramas: GHS08,GHS09
• Palavra indicadora: Danger
• Frases de perigo: H360Df,H362,H410
• Declarações de precaução: P202 - P260 - P263 - P264 - P273 - P308 + P313
• Classificações de perigo: Aquatic Chronic 1 - Lact. - Repr. 1B
• Código de classe de armazenamento: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable
• Equipamento de proteção individual: Eyeshields, Gloves, type N95 (US)