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品質等級
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)
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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.
其他客户在看
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)
Nuclear Respiratory Factor 1 Acting as an Oncoprotein Drives Estrogen-Induced Breast Carcinogenesis
Das J, et al.
Cells, 7(12), 234-234 (2018)
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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