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COO原产地证书/COA分析证书

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I4409

氟维司群

Name: 氟维司群
Brand: SIGMA

>98% (HPLC)

别名:

(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

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About This Item

经验公式（希尔记法）:

C₃₂H₄₇F₅O₃S

CAS Number:

129453-61-8

分子量:

606.77

MDL编号:

MFCD00903953

UNSPSC代码:

51111800

PubChem化学物质编号:

329815373

NACRES:

NA.77

质量水平

100

方案

>98% (HPLC)

表单

powder

溶解性

DMSO: >5 mg/mL

创始人

AstraZeneca

储存温度

2-8°C

SMILES字符串

[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 key

VWUXBMIQPBEWFH-WCCTWKNTSA-N

基因信息

human ... ESR1(2099), ESR2(2100)

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应用

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

氟维司群是一种选择性雌激素受体下调剂（SERD）；具有高亲和力的雌激素受体拮抗剂。

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.

特点和优势

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.