Accueil>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>Fulvestrant (ICI 182,780)

Fulvestrant (ICI 182,780) (Synonyms: ICI 182780)

Catalog No.GC18000

Fulvestrant est un antagoniste sélectif du récepteur des œstrogènes (ER). Il se lie, bloque et dégrade ER, puis inhibe l'activité transcriptionnelle médiée par ER avec une IC50 de 9,4 nM.

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Fulvestrant (ICI 182,780) Chemical Structure

Cas No.: 129453-61-8

Taille Prix Stock Qté
10mM (in 1mL DMSO)
37,00 $US
En stock
25mg
36,00 $US
En stock
100mg
69,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 4 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Bats-72 cell line (estrogen receptor-negative MDR cell line)

Preparation method

Cells were exposed to designated concentrations of doxorubicin with or without co-treatment of fulvestrant for 72 h, the cell viabilities were determined.

Reaction Conditions

1-10 µM;72 h

Applications

Fulvestrant sensitizes doxorubicin-induced cytotoxicity in estrogen receptor-negative MDR cell line Bats-72.

Animal experiment [2]:

Animal models

Balb/C-nu/nu mice (MCF7 cells model)

Preparation method

Mice were treated with fulvestrant in addition to the estradiol exposure.

Dosage form

5 mg/mouse; s.c.; twice per week

Applications

Fulvestrant significantly inhibited macrophage and neutrophil infiltration in mice cancer model.

References:

[1]. Huang Y, Jiang D,et,al. Fulvestrant reverses doxorubicin resistance in multidrug-resistant breast cell lines independent of estrogen receptor expression. Oncol Rep. 2017 Feb;37(2):705-712. doi: 10.3892/or.2016.5315. Epub 2016 Dec 14. PMID: 28000875; PMCID: PMC5355712.

[2]. Abrahamsson A, Rodriguez GV, et,al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. doi: 10.1158/0008-5472.CAN-20-1705. Epub 2020 Aug 27. PMID: 32855207.

Background

Fulvestrant est un antagoniste sélectif du récepteur des œstrogènes (ER). Il se lie, bloque et dégrade le récepteur des œstrogènes, puis inhibe l'activité transcriptionnelle médiée par le récepteur des œstrogènes (ER) avec une IC50 de 9,4 nM [1-3]. Fulvestrant (3 μM; 1 mois) augmente la sensibilité des cellules NSCLC H1975 au gefitinib[4]. Fulvestrant (1-10 µM; 72 h) a fortement sensibilisé la cytotoxicité induite par la doxorubicine dans les lignées cellulaires MDR[5]. Fulvestrant (5 mg/souris ; s.c. ; deux fois par semaine) a significativement inhibé l'infiltration de macrophages et de neutrophiles dans un modèle murin de cancer. Fulvestrant diminue la croissance du cancer du sein ER+ en présence de niveaux physiologiques d'estradiol chez les souris nues atteintes d'un cancer du sein humain[6]. La combinaison de fulvestrant (5mg/souris ; deux fois par semaine ; s.c.) avec tamoxifène a amélioré la régression tumorale[7].

References:
[1]. Vergote I, Robertson JF. Fulvestrant is an effective and well-tolerated endocrine therapy for postmenopausal women with advanced breast cancer: results from clinical trials. Br J Cancer. 2004 Mar;90 Suppl 1(Suppl 1):S11-4. doi: 10.1038/sj.bjc.6601631. PMID: 15094759; PMCID: PMC2750769.
[2]. Osborne CK, Wakeling A, et,al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1(Suppl 1):S2-6. doi: 10.1038/sj.bjc.6601629. PMID: 15094757; PMCID: PMC2750773.
[3]. Dowsett M, Nicholson RI, et,al. Biological characteristics of the pure antiestrogen fulvestrant: overcoming endocrine resistance. Breast Cancer Res Treat. 2005;93 Suppl 1:S11-8. doi: 10.1007/s10549-005-9037-3. PMID: 16247595.
[4]. Shen H, Liu J, et,al. Fulvestrant increases gefitinib sensitivity in non-small cell lung cancer cells by upregulating let-7c expression. Biomed Pharmacother. 2014 Apr;68(3):307-13. doi: 10.1016/j.biopha.2013.10.007. Epub 2013 Nov 7. PMID: 24268810.
[5]. Huang Y, Jiang D, et,al. Fulvestrant reverses doxorubicin resistance in multidrug-resistant breast cell lines independent of estrogen receptor expression. Oncol Rep. 2017 Feb;37(2):705-712. doi: 10.3892/or.2016.5315. Epub 2016 Dec 14. PMID: 28000875; PMCID: PMC5355712.
[6]. Abrahamsson A, Rodriguez GV, et,al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. doi: 10.1158/0008-5472.CAN-20-1705. Epub 2020 Aug 27. PMID: 32855207.
[7]. Mishra AK, Abrahamsson A, et,al. Fulvestrant inhibits growth of triple negative breast cancer and synergizes with tamoxifen in ERα positive breast cancer by up-regulation of ERβ. Oncotarget. 2016 Aug 30;7(35):56876-56888. doi: 10.18632/oncotarget.10871. PMID: 27486755; PMCID: PMC5302959.

Chemical Properties

Cas No. 129453-61-8 SDF
Synonymes ICI 182780
Chemical Name (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
Canonical SMILES CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
Formula C32H47F5O3S M.Wt 606.77
Solubility ≥ 30.35mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6481 mL 8.2404 mL 16.4807 mL
5 mM 0.3296 mL 1.6481 mL 3.2961 mL
10 mM 0.1648 mL 0.824 mL 1.6481 mL
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Review for Fulvestrant (ICI 182,780)

Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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