MW 606.8 Da, Purity >99%. Estrogen receptor antagonist with no partial agonist activity. Anticancer agent (IC50 = 0.29 nM for inhibition of breast cancer cell growth). Causes downregulation and loss of estrogen receptors.
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- Molecular therapy. Nucleic acids 29:836-8512022A novel oncogenic enhancer of estrogen receptor-positive breast cancer.Applications:Unspecified applicationReactive species:Unspecified reactive speciesChunjie Bao,Jialun Duan,Ying Xie,Yixuan Liu,Peishan Li,Jianwei Li,Huihui Zhao,Haitao Guo,Yanchen Men,Yuxin Ren,Jiarui Xu,Guiling Wang,Wanliang LuPubMed 36159594
- The Journal of biological chemistry 294:15577-15592201917β-Estradiol nongenomically induces vascular endothelial HS release by promoting phosphorylation of cystathionine γ-lyase.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXingyan Xu et. al.PubMed 31439665
- Reproductive biology and endocrinology : RB&E 17:12019Profile of melatonin and its receptors and synthesizing enzymes in cumulus-oocyte complexes of the developing sheep antral follicle-a potential estradiol-mediated mechanism.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLongfei Xiao et. al.PubMed 30606208
- Oncogene 38:1019-10372018Role of SUMOylation in differential ERα transcriptional repression by tamoxifen and fulvestrant in breast cancer cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTatiana Traboulsi,Mohamed El Ezzy,Vanessa Dumeaux,Eric Audemard,Sylvie MaderPubMed 30190545
- BMC complementary and alternative medicine 18:1072018The in vitro estrogenic activity of the crude drugs found in Japanese herbal medicines prescribed for menopausal syndrome was enhanced by combining them.Applications:Unspecified applicationReactive species:Unspecified reactive speciesZeyun Wang et. al.PubMed 29566679
- Scientific reports 7:84862017In vivo and in vitro sex differences in the dendritic morphology of developing murine hippocampal and cortical neurons.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKimberly P Keil et. al.PubMed 28814778
- PloS one 9:e958782014Induction of the CLOCK gene by E2-ERα signaling promotes the proliferation of breast cancer cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLiyun Xiao et. al.PubMed 24789043
- Journal of molecular endocrinology 51:1-132013A novel first exon directs hormone-sensitive transcription of the pig prolactin receptor.Applications:Unspecified applicationReactive species:Unspecified reactive speciesAnke Schennink et. al.PubMed 23576686
Key facts
- CAS number
- 129453-61-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 606.8 Da
- Molecular formula
- C32H47F5O3S
- PubChem identifier
- 17756771
- Nature
- Synthetic
Target data
Recommended products
MW 606.8 Da, Purity >99%. Estrogen receptor antagonist with no partial agonist activity. Anticancer agent (IC50 = 0.29 nM for inhibition of breast cancer cell growth). Causes downregulation and loss of estrogen receptors.
Key facts
- CAS number
- 129453-61-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 606.8 Da
- Molecular formula
- C32H47F5O3S
- PubChem identifier
- 17756771
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
Soluble in ethanol to 50 mM.
- Biochemical name
- (1S,9R,11S,14S,15S)-15-methyl-9-[9-(4,4,5,5,5-pentafluoropentanesulfinyl)nonyl]tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-triene-5,14-diol
- Biological description
Estrogen receptor antagonist with no partial agonist activity. Anticancer agent (IC50 = 0.29 nM for inhibition of breast cancer cell growth). Causes downregulation and loss of estrogen receptors.
- Canonical SMILES
- CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
- Isomeric SMILES
- C[C@]12CC[C@H]3C([C@@H]1CC[C@@H]2O)[C@@H](CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
- InChI
- InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29?,30+,41?/m1/s1
- InChIKey
- VWUXBMIQPBEWFH-LQKBAPIOSA-N
- IUPAC name
- (7R,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
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
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2 product images
Chemical Structure - ICI 182,780, Estrogen receptor antagonist (ab120131)
2D chemical structure image of ab120131, ICI 182,780, Estrogen receptor antagonist
Functional Studies - ICI 182,780, Estrogen receptor antagonist (ab120131)
ab47489 staining BCL2 in MCF7 cells treated with ICI 182,780 (ab120131), by ICC/IF. Decrease in BCL2 expression correlates with increased concentration of ICI 182,780 as described in literature.
The cells were incubated at 37°C for 3h in media containing different concentrations of ab120131 (ICI 182,780) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab47489 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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