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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Cas No.: 129453-61-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
Prepare stock solution | |||
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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