IF 11
Fulvestrant (ICI 182,780)
Catalog No.: GC18000Purity:>98.00%Synonyms: ICI 182780
Fulvestrant is a selective estrogen receptor (ER) antagonist. It binds, blocks and degrades estrogen receptor, then inhibits estrogen receptor(ER)-mediated transcriptional activity with an IC50 of 9.4 nM .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 129453-61-8
10mM (in 1mL DMSO)In Stock
$38.00
1
25mgIn Stock
$36.00
1
100mgIn Stock
$70.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $38.00 | In Stock | 1 | |
| 25mg | $36.00 | In Stock | 1 | |
| 100mg | $70.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
7 publicationsPublications from researchers using this productDescription
Fulvestrant is a selective estrogen receptor (ER) antagonist. It binds, blocks and degrades estrogen receptor, then inhibits estrogen receptor(ER)-mediated transcriptional activity with an IC50 of 9.4 nM [1-3].
Fulvestrant(3 μM ;1 month) increases the sensitivity of H1975 NSCLC cells to gefitinib[4].Fulvestrant(1-10 µM;72 h) strongly sensitized doxorubicin-induced cytotoxicity in MDR cell lines[5].
Fulvestrant(5 mg/mouse; s.c.; twice per week) significantly inhibited macrophage and neutrophil infiltration in mice cancer model. Fulvestrant decreases ER+ breast cancer growth in the presence of physiologic levels of estradiol in human breast cancer in nude mice[6]. Fulvestrant (5mg/mouse; twice weekly; s.c.) in combination with tamoxifen enhanced tumor regression[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.
Protocol
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Cell experiment [1]: |
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Cell lines |
Bats-72 cell line (estrogen receptor-negative MDR cell line) |
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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. |
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Reaction Conditions |
1-10 µM;72 h |
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Applications |
Fulvestrant sensitizes doxorubicin-induced cytotoxicity in estrogen receptor-negative MDR cell line Bats-72. |
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Animal experiment [2]: |
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Animal models |
Balb/C-nu/nu mice (MCF7 cells model) |
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Preparation method |
Mice were treated with fulvestrant in addition to the estradiol exposure. |
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Dosage form |
5 mg/mouse; s.c.; twice per week |
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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. |
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Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 3
Chemical Properties
CAS No.
129453-61-8
Synonyms
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
SMILES
CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
Molecular Formula
C32H47F5O3S
Molecular Weight
606.77
Solubility
≥ 30.35mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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