I4409

Fulvestrant

>98% (HPLC)

• Synonim(y): (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
• Wzór empiryczny (zapis Hilla): C₃₂H₄₇F₅O₃S
• Numer CAS: 129453-61-8
• Masa cząsteczkowa: 606.77
• Numer MDL: MFCD00903953
• Kod UNSPSC: 51111800
• Identyfikator substancji w PubChem: 329815373
• NACRES: NA.77

Właściwości

• Próba: >98% (HPLC)
• Formularz: powder
• rozpuszczalność: DMSO: >5 mg/mL
• inicjator: AstraZeneca
• temp. przechowywania: 2-8°C
• ciąg 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
• Klucz InChI: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• informacje o genach: human ... ESR1(2099) , ESR2(2100)

Opis

Zastosowanie

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

Działania biochem./fizjol.

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.

Cechy i korzyści

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.

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS08,GHS09
• Hasło ostrzegawcze: Danger
• Zwroty wskazujące rodzaj zagrożenia: H360Df,H362,H410
• Zwroty wskazujące środki ostrożności: P202 - P260 - P263 - P264 - P273 - P308 + P313
• Klasyfikacja zagrożeń: Aquatic Chronic 1 - Lact. - Repr. 1B
• Kod klasy składowania: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable
• Środki ochrony indywidualnej: Eyeshields, Gloves, type N95 (US)