ICI 182,780

Pricing Availability   Qty
Description: Estrogen receptor antagonist
Alternative Names: Fulvestrant
Chemical Name: 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Purity: ≥99% (HPLC)
Citations (284)
Reviews (1)
Pathways (1)

Biological Activity for ICI 182,780

ICI 182,780 is a high affinity estrogen receptor antagonist (IC50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo. ICI 182,780 is a high affinity agonist at the membrane estrogen receptor GPER. ICI 182,780 inhibits MCF-7 human breast cancer cell growth in vitro and shows antitumor activity in mice models. ICI 182,780 penetrates the blood-brain-barrier and has neuronal functional effects in vivo.

Compound Libraries for ICI 182,780

ICI 182,780 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for ICI 182,780

M. Wt 606.77
Formula C32H47F5O3S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 129453-61-8
PubChem ID 17756771
Smiles OC1=CC=C2C(C[C@@H](CCCCCCCCCS(CCCC(F)(C(F)(F)F)F)=O)C3([H])[C@@]([H])2CC[C@@]4(C)[C@@](CC[C@@H]4O)3[H])=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ICI 182,780

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 30.34 50
DMSO 60.68 100

Preparing Stock Solutions for ICI 182,780

The following data is based on the product molecular weight 606.77. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.65 mL 8.24 mL 16.48 mL
5 mM 0.33 mL 1.65 mL 3.3 mL
10 mM 0.16 mL 0.82 mL 1.65 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets for ICI 182,780

Certificate of Analysis / Product Datasheet
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References for ICI 182,780

References are publications that support the biological activity of the product.

de Cupis et al (1995) Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting OE and IGF-I induced proliferation of human breast cancer-derived cells. Br.J.Pharmacol. 116 2391 PMID: 8581274

Howell et al (2000) ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89 817 PMID: 10951345

Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 146 624 PMID: 15539556

Wakeling et al (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res. 51 3867 PMID: 1855205

Alfinito et al (2008) ICI 182,780 penetrates brain and hypothalamic tissue and has functional effects in the brain after systemic dosing. Endocrinology 149 5219 PMID: 18599545

If you know of a relevant reference for ICI 182,780, please let us know.

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Keywords: ICI 182,780, ICI 182,780 supplier, High, affinity, GPR30, agonist, Estrogen, receptors, antagonists, ER, ERR, ICI182780, AstraZeneca, GPER, antitumor, Fulvestrant, and, Related, Receptors, (GPER), 1047, Tocris Bioscience

284 Citations for ICI 182,780

Citations are publications that use Tocris products. Selected citations for ICI 182,780 include:

Panza et al (2017) E2 via estrogen receptor beta influences ROS levels through the transcriptional regulation of SIRT3 in human seminoma TCam-2 cells. Tumour Biol 39 1010428317701640 PMID: 28459202

Yi et al (2014) Anti-tumor efficacy of fulves. in estrogen receptor positive gastric cancer. Sci Rep 4 7592 PMID: 25534230

Adomas et al (2014) Breast tumor specific mutation in GATA3 affects physiological mechanisms regulating transcription factor turnover. BMC Cancer 14 278 PMID: 24758297

Giretti et al (2014) Effects of Estetrol on Migration and Invasion in T47-D Breast Cancer Cells through the Actin Cytoskeleton. Front Endocrinol (Lausanne) 5 80 PMID: 24904530

Hill and Muldrew (2014) Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries. Clin Exp Pharmacol Physiol 41 430 PMID: 24684418

Liang et al (2014) Egr1 protein acts downstream of estrogen-leukemia inhibitory factor (LIF)-STAT3 pathway and plays a role during implantation through targeting Wnt4. J Biol Chem 289 23534 PMID: 25012664

Colciago et al (2014) In vitro chronic administration of ERbeta selective ligands and prostate cancer cell growth: hypotheses on the selective role of 3beta-adiol in AR-positive RV1 cells. Biomed Res Int 2014 801473 PMID: 24877132

Oróstica et al (2014) OE increases cAMP in the oviductal secretory cells through a nongenomic mechanism. Reproduction 148 285 PMID: 25038866

Haagenson et al (2014) Functional analysis of MKP-1 and MKP-2 in breast cancer tamox. sensitivity. Oncotarget 5 1101 PMID: 24658355

Gottardo et al (2014) Antiapoptotic factor humanin is expressed in normal and tumoral pituitary cells and protects them from TNF-α-induced apoptosis. PLoS One 9 e111548 PMID: 25360890

Alao et al (2014) Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer 14 853 PMID: 25409876

Fan et al (2014) Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer 50 457 PMID: 24183378

Fan et al (2014) A molecular model for the mechanism of acquired tamox. resistance in breast cancer. Eur J Cancer 50 2866 PMID: 25204804

Chen et al (2008) Estrogen prevents intestinal inflammation after trauma-hemorrhage via downregulation of angiotensin II and angiotensin II subtype I receptor. J Mol Endocrinol 295 G1131 PMID: 18832446

Pan et al (2008) Differential expression of microRNAs in myometrium and leiomyomas and regulation by ovarian steroids. J Biol Chem 12 227 PMID: 18182067

Matsubara et al (2008) Estrogen determines sex differences in airway responsiveness after allergen exposure. Reprod Sci 38 501 PMID: 18063836

Toloubeydokhti et al (2008) The expression and ovarian steroid regulation of endometrial micro-RNAs. J Exp Clin Cancer Res 15 993 PMID: 19088369

Tsutsumi et al (2008) Differential regulation of the inducible nitric oxide synthase gene by estrogen receptors 1 and 2. Tissue Eng Part C Methods 199 267 PMID: 18753331

Sirianni et al (2008) The novel estrogen receptor, G protein-coupled receptor 30, mediates the proliferative effects induced by 17β-OE on mouse spermatogonial GC-1 cell line. Int J Oncol 149 5043 PMID: 18566133

Albanito et al (2008) G-protein-coupled receptor 30 and estrogen receptor-alpha are involved in the proliferative effects induced by atrazine in ovarian cancer cells. Environ Health Perspect 116 1648 PMID: 19079715

Galluzzo et al (2008) The nutritional flavanone naringenin triggers antiestrogenic effects by regulating estrogen receptor alpha-palmitoylation. Endocrinology 149 2567 PMID: 18239068

Iorns et al (2008) Identification of CDK10 as an important determinant of resistance to endocrine therapy for breast cancer. Cancer Cell 13 91 PMID: 18242510

Yuan et al (2008) Effects of OE and progesterone on the proinflammatory cytokine production by mononuclear cells from patients with chronic hepatitis C. World J Gastroenterol 14 2200 PMID: 18407594

Wang et al (2008) Hormonal regulation of BCRP expression in human placental BeWo cells. Pharm Res 25 444 PMID: 17823853

Subtil-Rodríguez et al (2008) Progesterone induction of the 11beta-hydroxysteroid dehydrogenase type 2 promoter in breast cancer cells involves coordinated recruitment of STAT5A and progesterone receptor to a distal enhancer and polymerase tracking. Mol Cell Biol 28 3830 PMID: 18378698

Teng et al (2008) Roles of estrogen receptor alpha and beta in modulating urothelial cell proliferation. Endocr Relat Cancer 15 351 PMID: 18310301

Liu et al (2008) Estrogen-enhanced gene expression of lipoprotein lipase in heart is antagonized by progesterone. Endocrinology 149 711 PMID: 17974624

Oh et al (2008) Tyrosine phosphorylation of the nuclear receptor coactivator AIB1/SRC-3 is enhanced by Abl kinase and is required for its activity in cancer cells. Mol Cell Biol 28 6580 PMID: 18765637

Cortes et al (2019) TAX mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival. EMBO Rep 20 PMID: 30538116

Cortes et al (2019) GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment. EMBO Rep 20 PMID: 30538117

Wong et al (2017) Role of inducible nitric oxide synthase in endothelium-independent relaxation to RLX in rat aorta. Br J Pharmacol 174 718 PMID: 28138957

Speroni et al (2014) Hormonal regulation of epithelial organization in a three-dimensional breast tissue culture model. PLoS One 20 42 PMID: 23675751

Choi et al (2014) Suppression of autophagic activation in the mouse uterus by estrogen and progesterone. Cell Rep 221 39 PMID: 24443716

Seo et al (2014) Comprehensive analysis of prostaglandin metabolic enzyme expression during pregnancy and the characterization of AKR1B1 as a prostaglandin F synthase at the maternal-conceptus interface in pigs. Breast Cancer Res 90 99 PMID: 24695626

Teng et al (2013) Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells. Toxicol Sci 131 71 PMID: 23052036

Johansson et al (2013) Retinoic acid receptor alpha is associated with tamox. resistance in breast cancer. Nat Commun 4 2175 PMID: 23868472

Greaves et al (2013) ERβ-dependent effects on uterine endothelial cells are cell specific and mediated via Sp1. Hum Reprod 28 2490 PMID: 23756706

Morandi et al (2013) GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res 73 3783 PMID: 23650283

Thangavel et al (2011) Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer 18 333 PMID: 21367843

Lee et al (2009) K+-dependent Na+/Ca2+ exchanger 3 is involved in renal active calcium transport and is differentially expressed in the mouse kidney. Am J Physiol Renal Physiol 297 F371 PMID: 19474185

Han et al (2009) The estrogen receptor alpha pathway induces oncogenic Wip1 phosphatase gene expression. Mol Cancer Res 7 713 PMID: 19435816

Iorns et al (2009) CRK7 modifies the MAPK pathway and influences the response to endocrine therapy. Carcinogenesis 30 1696 PMID: 19651820

Flamini et al (2009) Differential actions of estrogen and SERMs in regulation of the actin cytoskeleton of endometrial cells. Mol Hum Reprod 15 675 PMID: 19541800

Schaub and Wood (2009) Blockade of estrogen action upregulates estrogen receptor-alpha mRNA in the fetal brain. Neonatology 96 115 PMID: 19279395

Tan et al (2009) Autocrine regulation of cell proliferation by estrogen receptor-alpha in estrogen receptor-alpha-positive breast cancer cell lines. BMC Cancer 9 31 PMID: 19171042

Comitato et al (2009) A novel mechanism of natural vitamin E tocotrienol activity: involvement of ERbeta signal transduction. Am J Physiol Endocrinol Metab 297 E427 PMID: 19491296

Boue et al (2009) Identification of the potent phytoestrogen glycinol in elicited soybean (Glycine max). Endocrinology 150 2446 PMID: 19116342

Hsieh et al (2009) Mechanism of the salutary effects of estrogen on kupffer cell phagocytic capacity following trauma-hemorrhage: pivotal role of Akt activation. J Immunol 182 4406 PMID: 19299741

Chisamore et al (2009) Characterization of a novel small molecule subtype specific estrogen-related receptor alpha antagonist in MCF-7 breast cancer cells. PLoS One 4 e5624 PMID: 19462000

Quiles et al (2009) Mutational analysis of progesterone receptor functional domains in stable cell lines delineates sets of genes regulated by different mechanisms. Mol Endocrinol 23 809 PMID: 19299443

Park et al (2009) 17Beta-OE at low concentrations acts through distinct pathways in normal versus benign prostatic hyperplasia-derived prostate stromal cells. Endocrinology 150 4594 PMID: 19608654

Bolanz et al (2009) Tamoxifen inhibits TRPV6 activity via estrogen receptor-independent pathways in TRPV6-expressing MCF-7 breast cancer cells. Mol Cancer Res 7 2000 PMID: 19996302

Hartman et al (2009) Hes-6, an inhibitor of Hes-1, is regulated by 17β-OE and promotes breast cancer cell proliferation. Arthritis Res Ther 11 R79 PMID: 19891787

Kramár et al (2009) Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity. Hum Mol Genet 29 12982 PMID: 19828812

Vedin et al (2009) The oxysterol receptor LXR inhibits proliferation of human breast cancer cells. Cancer Res 30 575 PMID: 19168586

Bondar et al (2009) OE-induced estrogen receptor-α trafficking. Mol Cell Endocrinol 29 15323 PMID: 19955385

Demas et al (2019) Glutamine Metabolism Drives Growth in Advanced Hormone Receptor Positive Breast Cancer. Front Oncol 9 686 PMID: 31428575

Bloomfield and Louie (2019) Chronic cadmium exposure decreases the dependency of MCF7 breast cancer cells on ERα. Sci Rep 9 12135 PMID: 31431634

Rincó n-Rodriguez et al (2019) F-Spondin Is the Signal by Which 2-Methoxyestradiol Induces Apoptosis in the Endometrial Cancer Cell Line Ishikawa. Int J Mol Sci 20 PMID: 31394756

Hosford et al (2019) Estrogen therapy induces an unfolded protein response to drive cell death in ER+ breast cancer. Mol Oncol 13 1778 PMID: 31180176

Kasonga et al (2019) Data on UPLC/MS method validation for the biodegradation of pharmaceuticals and intermediates by a fungal consortium and on T47DK-Bluc reporter gene assay to assess the reduction of their estrogenic activity. Data Brief 25 104336 PMID: 31453302

Cortes et al (2019) TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor. Oncogene 38 2910 PMID: 30575816

Lou et al (2017) OE Suppresses TLR4-triggered Apoptosis of Decidual Stromal Cells and Drives an Anti-inflammatory TH2 Shift by Activating SGK1. Int J Biol Sci 13 434 PMID: 28529452

Lu et al (2017) Estrogen enhances mismatch repair by induction of MLH1 expression via estrogen receptor-β. Oncotarget 8 38767 PMID: 28404976

Stender (2017) Structural and molecular mechanisms of cytokine-mediated endocrine resistance in human breast cancer cells. Mol Cell 65 1122 PMID: 28306507

Zhu (2017) Differential and directional estrogenic signaling pathways induced by enterolignans and their precursors. PLoS One 12 e0171390 PMID: 28152041

Wu et al (2015) Effects of estrogen on growth and smooth muscle differentiation of vascular wall-resident CD34(+) stem/progenitor cells. Atherosclerosis 240 453 PMID: 25898000

Wardell et al (2015) Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr Relat Cancer 22 713 PMID: 26162914

Lappano et al (2011) The cholesterol metabolite 25-hydroxycholesterol activates estrogen receptor α-mediated signaling in cancer cells and in cardiomyocytes. PLoS One 6 e16631 PMID: 21304949

Richardson et al (2011) Estrogen protection in Friedreich's ataxia skin fibroblasts. Endocrinology 152 2742 PMID: 21540287

Liu et al (2011) Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal mor. antinociception. J Neurosci 31 11836 PMID: 21849544

Shanle et al (2011) Generation of stable reporter breast cancer cell lines for the identification of ER subtype selective ligands. Biochem Pharmacol 82 1940 PMID: 21924251

Belcher et al (2009) Blockade of estrogen receptor signaling inhibits growth and migration of medulloblastoma. Endocrinology 150 1112 PMID: 19008315

Valeri et al (2009) Effects of 17beta-oOE on rat detrusor smooth muscle contractility. Exp Physiol 94 834 PMID: 19395661

Rogers et al (2009) OE stimulates Akt, AMP-activated protein kinase (AMPK) and TBC1D1/4, but not glucose uptake in rat soleus. Biochem Biophys Res Commun 382 646 PMID: 19265681

Dickerson et al (2009) Cell death mechanisms in GT1-7 GnRH cells exposed to polychlorinated biphenyls PCB74, PCB118, and PCB153. Toxicol Appl Pharmacol 237 237 PMID: 19362103

Schreihofer and Redmond (2009) Soy phytoestrogens are neuroprotective against stroke-like injury in vitro. Neuroscience 158 602 PMID: 18976694

Peretz et al (2016) Estrogenic compounds reduce influenza A virus replication in primary human nasal epithelial cells derived from female, but not male, donors. Am J Physiol Lung Cell Mol Physiol 310 L415 PMID: 26684252

Shappell et al (2015) The Effects of Steroid Implant and Dietary Soybean Hulls on Estrogenic Activity of Sera of Steers Grazing Toxic Endophyte-Infected Tall Fescue Pasture. Cancer Lett 2 30 PMID: 26664959

Wang et al (2015) Differential effects of estrogen and estrogen receptor antagonist, ICI 182 780, on the expression of calbindin-D9k in rat pituitary prolactinoma GH3 cells. Cancer Cell Int 7 8498 PMID: 25674214

Zhou et al (2015) Estrogen mediated expression of nucleophosmin 1 in human endometrial carcinoma clinical stages through estrogen receptor-α signaling. Endocrinology 14 540 PMID: 25663821

Simões et al (2015) Anti-estrogen Resistance in Human Breast Tumors Is Driven by JAG1-NOTCH4-Dependent Cancer Stem Cell Activity. Cell Cycle 12 1968 PMID: 26387946

Hole et al (2015) New cell culture model for aromatase inhibitor-resistant breast cancer shows sensitivity to fulves. treatment and cross-resistance between letr. and exeme. BMC Cancer 46 1481 PMID: 25625755

Larsen et al (2015) Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamox. resistant breast cancer. Aging Cell 15 239 PMID: 25885472

Xiong et al (2015) Opposite effects of two estrogen receptors on tau phosphorylation through disparate effects on the miR-218/PTPA pathway. Breast Cancer Res Treat 14 867 PMID: 26111662

Bean et al (2015) The PI3K/mTOR dual inhibitor P7170 demonstrates potent activity against endocrine-sensitive and endocrine-resistant ER+ breast cancer. Oncotarget 149 69 PMID: 25491778

Luzhna et al (2015) Altered radiation responses of breast cancer cells resistant to hormonal therapy. Mol Cell Biol 6 1678 PMID: 25682200

Hu et al (2015) NF-κB signaling is required for XBP1 (unspliced and spliced)-mediated effects on antiestrogen responsiveness and cell fate decisions in breast cancer. Oncogenesis 35 379 PMID: 25368386

Miyoshi et al (2015) Nodes-and-connections RNAi knockdown screening: identification of a signaling molecule network involved in fulves. action and breast cancer prognosis. Biol Sex Differ 4 e172 PMID: 26479444

Myers et al (2015) Estrogenic and anti-estrogenic activity of off-the-shelf hair and skin care products. BMC Cancer 25 271 PMID: 24849798

Segovia-Mendoza et al (2015) Antihormonal agents as a strategy to improve the effect of chemo-radiation in cervical cancer: in vitro and in vivo study. J Biol Chem 15 21 PMID: 25622528

Varea et al (2013) OOE signalling through the Akt-mTORC1-S6K1. Biochim Biophys Acta 1833 1052 PMID: 23295457

Spink et al (2013) Expression of the aryl hydrocarbon receptor is not required for the proliferation, migration, invasion, or estrogen-dependent tumorigenesis of MCF-7 breast cancer cells. Mol Carcinog 52 544 PMID: 22388733

Giordano et al (2013) Gender differences in brain susceptibility to oxidative stress are mediated by levels of paraoxonase-2 expression. Free Radic Biol Med 58 98 PMID: 23376469

Smith et al (2013) The membrane estrogen receptor ligand STX rapidly enhances GABAergic signaling in NPY/AgRP neurons: role in mediating the anorexigenic effects of 17β-OE. Am J Physiol Endocrinol Metab 305 E632 PMID: 23820624

Brion et al (2012) Screening estrogenic activities of chemicals or mixtures in vivo using transgenic (cyp19a1b-GFP) zebrafish embryos. PLoS One 7 e36069 PMID: 22586461

Zhang et al (2012) Estrogen-responsive nitroso-proteome in uterine artery endothelial cells: role of endothelial nitric oxide synthase and estrogen receptor-β. J Cell Physiol 227 146 PMID: 21374595

Antoon et al (2010) Antiestrogenic effects of the novel sphingosine kinase-2 inhibitor ABC294640. Endocrinology 151 5124 PMID: 20861237

Sobrino et al (2010) OE selectively stimulates endothelial prostacyclin production through estrogen receptor-{alpha}. J Mol Endocrinol 44 237 PMID: 20110403

Yang et al (2010) Extranuclear estrogen receptors mediate the neuroprotective effects of estrogen in the rat hippocampus. PLoS One 5 e9851 PMID: 20479872

Raffetto et al (2010) Estrogen receptor-mediated enhancement of venous relaxation in female rat: implications in sex-related differences in varicose veins. J Vasc Surg 51 972 PMID: 20347696

Ma et al (2010) Gender-specific reduction in contraction is associated with increased estrogen receptor expression in single vascular smooth muscle cells of female rat. Cell Physiol Biochem 26 457 PMID: 20798531

Si (2009) Isoflavone genistein protects human vascular endothelial cells against tumor necrosis factor-alpha-induced apoptosis through the p38beta mitogen-activated protein kinase. Apoptosis 14 66 PMID: 19082897

Miyakoshi et al (2009) The expression of Wnt4 is regulated by estrogen via an estrogen receptor alpha-dependent pathway in rat pituitary GH-producing cells. Acta Histochem Cytochem 42 205 PMID: 20126574

Zhang et al (2009) Estrogen attenuates ischemic oxidative damage via an estrogen receptor alpha-mediated inhibition of NADPH oxidase activation. J Neurosci 29 13823 PMID: 19889994

Leung et al (2009) Protopanaxadiol and protopanaxatriol bind to glucocorticoid and oestrogen receptors in endothelial cells. Br J Pharmacol 156 626 PMID: 19226254

Ulhaq and Kishida (2018) Brain Aromatase Modulates Serotonergic Neuron by Regulating Serotonin Levels in Zebrafish Embryos and Larvae. Front Endocrinol (Lausanne) 9 230 PMID: 29867763

Li et al (2018) Upregulation of IRS1 Enhances IGF1 Response in Y537S and D538G ESR1 Mutant Breast Cancer Cells. Endocrinology 159 285 PMID: 29029116

Simões et al (2018) Estrogenicity of essential oils is not required to relieve symptoms of urogenital atrophy in breast cancer survivors. Ther Adv Med Oncol 10 1758835918766180 PMID: 29636827

Rabaglino et al (2018) A transcriptomics model of estrogen action in the ovine fetal hypothalamus: evidence for estrogenic effects of ICI 182,780. Physiol Rep 6 e13871 PMID: 30221477

Pastore et al (2016) Identification of Differential ER-Alpha Versus ER-Beta Mediated Activation of eNOS in Ovine Uterine Artery Endothelial Cells. Biol Reprod 94 139 PMID: 27170438

Gupta et al (2016) NCOA3 coactivator is a transcriptional target of XBP1 and regulates PERK-eIF2α-ATF4 signalling in breast cancer. Oncogene 35 5860 PMID: 27109102

Bains and Roberts (2016) Estrogen protects against DA neuron toxicity in primary mesencephalic cultures through an indirect P13K/Akt mediated astrocyte pathway. Neurosci Lett 610 79 PMID: 26520464

Yonova et al (2014) Diaryl and heteroaryl sulfides: synthesis via sulfenyl chlorides and evaluation as selective anti-breast-cancer agents. J Org Chem 79 1947 PMID: 24564865

Thuillier et al (2010) Interdependence of platelet-derived growth factor and estrogen-signaling pathways in inducing neonatal rat testicular gonocytes proliferation. Biol Reprod 82 825 PMID: 20089883

Mao et al (2010) Progesterone increases systemic and local uterine proportions of CD4+CD25+ Treg cells during midterm pregnancy in mice. Endocrinology 151 5477 PMID: 20844003

Suzuki et al (2010) Down-regulation of PROS1 gene expression by 17beta-OE via estrogen receptor alpha (ERalpha)-Sp1 interaction recruiting receptor-interacting protein 140 and the corepressor-HDAC3 complex. J Biol Chem 285 13444 PMID: 20200160

Dalvai and Bystricky (2010) Cell cycle and anti-estrogen effects synergize to regulate cell proliferation and ER target gene expression. PLoS One 5 e11011 PMID: 20543978

Mahmoodzadeh et al (2010) 17beta-OE inhibits matrix metalloproteinase-2 transcription via MAP kinase in fibroblasts. Cardiovasc Res 85 719 PMID: 19861308

Madeo et al (2010) c-Jun activation is required for 4-hydroxytamoxifen-induced cell death in breast cancer cells. Oncogene 29 978 PMID: 19935718

Murphy et al (2010) OE suppresses NF-kappa B activation through coordinated regulation of let-7a and miR-125b in primary human macrophages. J Immunol 184 5029 PMID: 20351193

Pradhan et al (2010) Proinflammatory cytokines enhance estrogen-dependent expression of the multidrug transporter gene ABCG2 through estrogen receptor and NF{kappa}B cooperativity at adjacent response elements. J Biol Chem 285 31100 PMID: 20705611

Sunters et al (2010) Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of Ins-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-i J Biol Chem 285 8743 PMID: 20042609

Sherrill et al (2010) Developmental exposures of male rats to soy isoflavones impact Leydig cell differentiation. Biol Reprod 83 488 PMID: 20554919

Diep et al (2016) Progesterone induces progesterone receptor gene (PGR) expression via rapid activation of protein kinase pathways required for cooperative estrogen receptor alpha (ER) and progesterone receptor (PR) genomic action at ER/PR target genes. Steroids 114 48 PMID: 27641443

Ciucci et al (2016) Multiple direct and indirect mechanisms drive estrogen-induced tumor growth in high grade serous ovarian cancers. Oncotarget 7 8155 PMID: 26797759

Mao et al (2016) Antiestrogen resistant cell lines expressing estrogen receptor α mutations upregulate the unfolded protein response and are killed by BHPI Scientific Reports 6 34753 PMID: 27713477

Jafaar et al (2014) β-D-glucan inhibits endocrine-resistant breast cancer cell proliferation and alters gene expression. Int J Oncol 44 1365 PMID: 24534923

Rodriguez-Ubreva et al (2012) Pre-B cell to macrophage transdifferentiation without significant promoter DNA methylation changes. Nucleic Acids Res 40 1954 PMID: 22086955

González-Arenas et al (2012) OE increases cell growth in human astrocytoma cell lines through ERα activation and its interaction with SRC-1 and SRC-3 coactivators. Biochim Biophys Acta 1823 379 PMID: 22142990

Collins-Burow et al (2012) Antiestrogenic activity of flavonoid phytochemicals mediated via the c-Jun N-terminal protein kinase pathway. Cell-type specific regulation of estrogen receptor alpha. J Steroid Biochem Mol Biol 132 186 PMID: 22634477

Peretz et al (2012) Bisphenol A inhibits follicle growth and induces atresia in cultured mouse antral follicles independently of the genomic estrogenic pathway. Biol Reprod 87 63 PMID: 22743301

Leal et al (2012) p130Cas over-expression impairs mammary branching morphogenesis in response to estrogen and EGF. PLoS One 7 e49817 PMID: 23239970

Shim and Lee (2012) Estrogen receptor is activated by korean red ginseng in vitro but not in vivo. J Ginseng Res 36 169 PMID: 23717117

Cao et al (2012) Estrogen receptor β activation is antinociceptive in a model of visceral pain in the rat. J Pain 13 685 PMID: 22698981

Youn et al (2012) Inhibition of XO or NOX attenuates diethylstilbestrol-induced endothelial nitric oxide deficiency without affecting its effects on LNCaP cell invasion and apoptosis. Clin Sci (Lond) 123 509 PMID: 22568671

Antoon et al (2012) Inhibition of p38-MAPK alters SRC coactivation and estrogen receptor phosphorylation. Cancer Biol Ther 13 1026 PMID: 22825349

Babu et al (2012) Genistein prevents hyperglycemia-induced monocyte adhesion to human aortic endothelial cells through preservation of the cAMP signaling pathway and ameliorates vascular inflammation in obese diabetic mice. J Nutr 142 724 PMID: 22399524

Wang and Kuehl-Kovarik (2012) OE directly attenuates sodium currents and depolarizing afterpotentials in isolated gonadotropin-releasing hormone neurons. Brain Res 1436 81 PMID: 22209345

Ropero et al (2012) Insotropic effect of the non-steroidal compound STX in pancreatic β-cells. PLoS One 7 e34650 PMID: 22506040

Mahmoodzadeh et al (2012) 17β-OE-induced interaction of ERα with NPPA regulates gene expression in cardiomyocytes. Cardiovasc Res 96 411 PMID: 22962310

Bobustuc et al (2012) MGMT inhibition restores ERα functional sensitivity to antiestrogen therapy. Mol Med 18 913 PMID: 22549111

Wen et al (2012) Modulation of ovine SBD-1 expression by 17beta-OE in ovine oviduct epithelial cells. BMC Vet Res 8 143 PMID: 22920556

Rangasamy et al (2010) Estrogen suppresses MLK3-mediated apoptosis sensitivity in ER+ breast cancer cells. Cancer Res 70 1731 PMID: 20145118

Peng et al (2010) Unexpected hormonal activity of a catechol equine estrogen metabolite reveals reversible glutathione conjugation. Chem Res Toxicol 23 1374 PMID: 20540524

Lin et al (2010) B7-H1-dependent sex-related differences in tumor immunity and immunotherapy responses. J Immunol 185 2747 PMID: 20686128

Sanchez et al (2010) Estrogen receptor-alpha promotes breast cancer cell motility and invasion via focal adhesion kinase and N-WASP. Mol Endocrinol 24 2114 PMID: 20880986

Allard and Colaiácovo (2010) Bisphenol A impairs the double-strand break repair machinery in the germline and causes chromosome abnormalities. Proc Natl Acad Sci U S A 107 20405 PMID: 21059909

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Corcoran et al (2011) The effect of 17β-OE on cholesterol content in human macrophages is influenced by the lipoprotein milieu. Clin Cancer Res 47 109 PMID: 21830321

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Albanito et al (2015) Effects of Atrazine on Estrogen Receptor α- and G Protein-Coupled Receptor 30-Mediated Signaling and Proliferation in Cancer Cells and Cancer-Associated Fibroblasts. Environ Health Perspect 123 493 PMID: 25616260

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Aida-Yasuoka et al (2013) OE promotes the development of a fibrotic phenotype and is increased in the serum of patients with systemic sclerosis. J Neurosci 15 R10 PMID: 23305385

Zhang et al (2013) Fulvestrant regulates epidermal growth factor (EGF) family ligands to activate EGF receptor (EGFR) signaling in breast cancer cells. Environ Health Perspect 139 351 PMID: 23686416

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Zheng et al (2011) 17β-OE enhances breast cancer cell motility and invasion via extra-nuclear activation of actin-binding protein ezrin. PLoS One 6 e22439 PMID: 21818323

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Jover-Mengual et al (2007) MAPK signaling is critical to OE protection of CA1 neurons in global ischemia. Endocrinology 148 1131 PMID: 17138646

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Dalenc et al (2006) Farnesyl-transferase inhibitor R115,777 enhances tamox. inhibition of MCF-7 cell growth through estrogen receptor dependent and independent pathways. Breast Cancer Res 7 R1159 PMID: 16457696

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Chen et al (2006) Activation of Ins-like growth factor I receptor-mediated pathway by ginsenoside Rg1. Br J Pharmacol 147 542 PMID: 16415910

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Plísková et al (2005) Deregulation of cell proliferation by polycyclic aromatic hydrocarbons in human breast carcinoma MCF-7 cells reflects both genotoxic and nongenotoxic events. Toxicol Sci 83 246 PMID: 15548639

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Kendall et al (2005) Gonadal steroids differentially modulate neurotoxicity of HIV and cocaine: testost. and ICI 182,780 sensitive mechanism. BMC Neurosci 6 40 PMID: 15943860

Crane-Godreau and Wira (2005) Effects of OE on lipopolysaccharide and Pam3Cys stimulation of CCL20/macrophage inflammatory protein 3 α and tumor necrosis factor α production by uterine epithelial cells in culture. Breast Cancer Res Treat 73 4231 PMID: 15972514

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Ohshiro et al (2006) Biological role of estrogen receptor β in salivary gland adenocarcinoma cells. Exp Ther Med 12 5994 PMID: 17062671

Shih et al (2006) 17β-OE inhibits subarachnoid hemorrhage-induced inducible nitric oxide synthase gene expression by interfering with the nuclear factor κ B transactivation. Proc Natl Acad Sci U S A 37 3025 PMID: 17053178

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Used on human primary mammary epithelial cells.
By Anonymous on 04/18/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Human Primary Mammary Epithelial Cells

This product was dissolved in ethanol and delivered to human primary mammary epithelial cells in vitro.

Pathways for ICI 182,780

Estrogen Signaling Pathway

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.