Name: Fulvestrant (ICI 182,780)
Brand: GlpBio
SKU: GC18000
Availability: InStock
Rating: 5 (22 reviews)

Product has been cited by 4 publications

Related Biological Data

The change fold of (A) T, (B) 11-KT, (C) 17β-E2, (D) VTG in plasma of male and female zebrafish in dienestrol (ER agonist), fulvestral (ER antagonist),dihydrotestosterone (AR agonist), flutamide (AR antagonist) and different EHDPHP treatment groups (2.5, 50, 250 μg/L) compared with the control group (treated with 0.01% DMSO) and the values are expressed as mean ± standard error.
The concentration of DHT,DIES, FLU and FUL (Glpbio)was set at 10 nM.
Environment International 158 (2022): 106928. PMID: 34638023 IF: 9.623
Related Biological Data

E2 decreases neutrophils in c-mybhyper transgenic zebrafish embryos through ERs-independent mechanisms. G ICI 182780 did not alleviate E2-mediated inhibition of c-mybhyper zebrafish neutrophils.
The following compounds were used:DMSO; 17β-estradiol; 2,3-bis(4-hydroxyphenyl) propionitrile (DPN:50 μM, glpbio, GC17688); propyl pyrazole triol (PPT: 50 μM, glpbio, GC14370); fulvestrant (ICI-182,780:15 μM, glpbio, GC18000), G1 , E2 ELISA kit and PX-478 or compounds from the compound library.
Cell Death Discovery 8.1 (2022): 1-12. PMID: 35842445 IF: 7.1089
Related Biological Data

The e ects of ICI182780 treatment on the mRNA expression of Akt and β-catenin.
For ERα blocking test, the culture system on day 7 was treated with either placebo or 200 nM ICI182780 (GlpBio, co., Ltd., Montclair, NJ, USA) to block ERα pathways.
Int J Env Res Pub He 16.19 (2019): 3779. PMID: 31597358 IF: 2.007

Product Documents

Quality Control & SDS

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Purity: >99.50%

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.

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.

Cas No.	129453-61-8	SDF
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
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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Fulvestrant (ICI 182,780) (Synonyms: ICI 182780)

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Product has been cited by 4 publications

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Quality Control & SDS

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Complete Stock Solution Preparation Table

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In vivo Formulation Calculator (Clear solution)

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