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Merck
CN

I4409

Sigma-Aldrich

氟维司群

>98% (HPLC), PKC activator, powder

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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关于此项目

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

主要文件

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Product Name

氟维司群, >98% (HPLC)

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.

象形图

Health hazardEnvironment
GHS08,GHS09

警示用语：

Danger

危险声明

H360Df,H362,H410

危险分类

Aquatic Chronic 1 - Lact. - Repr. 1B

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

法规信息

监管及禁止进口产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000472079
0000472079
0000457709
0000457709
0000397621

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Nuclear Respiratory Factor 1 Acting as an Oncoprotein Drives Estrogen-Induced Breast Carcinogenesis
Das J, et al.
Cells, 7(12), 234-234 (2018)
Glutamic acid ameliorates estrogen deficiency-induced menopausal-like symptoms in ovariectomized mice
Han NR, et al.
Nutrition Research (New York, N.Y.), 35(9), 774-783 (2015)
Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action
Osborne CK, et al.
British Journal of Cancer, 90(S1), S2-S2 (2004)
Partial hepatectomy induces delayed hepatocyte proliferation and normal liver regeneration in ovariectomized mice
Umeda M, et al.
Clinical and Experimental Gastroenterology, 8(2), 175-175 (2015)
Manuele G Muraro et al.
Oncoimmunology, 6(7), e1331798-e1331798 (2017-08-16)
Interaction between cancerous, non-transformed cells, and non-cellular components within the tumor microenvironment plays a key role in response to treatment. However, short-term culture or xenotransplantation of cancer specimens in immunodeficient animals results in dramatic modifications of the tumor microenvironment, thus
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