I4409

氟维司群

>98% (HPLC)

• 同義詞: (7α,17β)-7-[9-[(4,4,5,5,5-五氟戊基)亚磺酰基]壬基]雌-1,3,5(10)-三烯-3,17-二醇, ICI 182,780, ZD 182780, ZD 9238, ZM 182780, 与法洛德
• 經驗公式（希爾表示法）: C₃₂H₄₇F₅O₃S
• CAS號碼: 129453-61-8
• 分子量：: 606.77
• MDL號碼: MFCD00903953
• 分類程式碼代碼: 51111800
• PubChem物質ID: 329815373
• NACRES: NA.77

屬性

• 化驗: >98% (HPLC)
• 形狀: powder
• 溶解度: DMSO: >5 mg/mL
• 起源: AstraZeneca
• 儲存溫度: 2-8°C
• SMILES 字串: [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
• InChI 密鑰: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• 基因資訊: human ... ESR1(2099) , ESR2(2100)

描述

應用

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

生化／生理作用

氟维司群（ICI 182,780）是一种选择性雌激素受体下调剂（SERD）。氟维司群是一种具有高亲和力的雌激素受体拮抗剂。IC₅₀ = 0.29 nM。氟维司群是第一种“纯”抗雌激素，在体外和体内均无激动活性。

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.

特點和優勢

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.

安全資訊

• 危險聲明: H413
• 防範說明: P273
• 危險分類: Aquatic Chronic 4
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 個人防護裝備: Eyeshields, Gloves, type N95 (US)