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Merck
CN

I4409

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
化学文摘社编号:
129453-61-8
分子量:
606.77
UNSPSC Code:
51111800
PubChem Substance ID:
329815373
NACRES:
NA.77
MDL number:
MFCD00903953

主要文件

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产品名称

氟维司群, >98% (HPLC)

SMILES string

[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

assay

>98% (HPLC)

form

powder

solubility

DMSO: >5 mg/mL

originator

AstraZeneca

storage temp.

2-8°C

Quality Level

100

Gene Information

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

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相关类别

Biochem/physiol Actions

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.

Application

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

Features and Benefits

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.

pictograms

Health hazardEnvironment
GHS08,GHS09

signalword

Danger

Hazard Classifications

Aquatic Chronic 1 - Lact. - Repr. 1B

存储类别

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

监管及禁止进口产品
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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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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, a new treatment option for advanced breast cancer: tolerability versus existing agents
Vergote I and Abram P
Annals of Oncology, 17(2), 200-204 (2005)
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
Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action
Osborne CK, et al.
British Journal of Cancer, 90(S1), S2-S2 (2004)
Nuclear Respiratory Factor 1 Acting as an Oncoprotein Drives Estrogen-Induced Breast Carcinogenesis
Das J, et al.
Cells, 7(12), 234-234 (2018)
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