ICI 182,780, Estrogen receptor antagonist (ab120131)
Key features and details
- Estrogen receptor antagonist
- CAS Number: 129453-61-8
- Soluble in DMSO to 100 mM and in ethanol to 50 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
ICI 182,780, Estrogen receptor antagonist -
Description
Estrogen receptor antagonist -
Alternative names
- Fulvestrant
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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.
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CAS Number
129453-61-8 -
Chemical structure
Properties
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Chemical name
(7R,9S,13S,14S,17S)-7-(9-(4,4,5,5,5-Pentafluoropentylsulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-13-methyl-6H-cyclopenta[a]phenanthrene-3,17-diol -
Molecular weight
606.77 -
Molecular formula
C32H47F5O3S -
PubChem identifier
17756771 -
Storage instructions
Store at Room Temperature. The product can be stored for up to 12 months. -
Solubility overview
Soluble in DMSO to 100 mM and in ethanol to 50 mM -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCC[C@@H]2Cc1cc(O)ccc1[C@H]3CC[C@]4(C)[C@@H](O)CC[C@H]4C23 -
Source
Synthetic
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Research areas
Applications
The Abpromise guarantee
Our Abpromise guarantee covers the use of ab120131 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
| Application | Abreviews | Notes |
|---|---|---|
| Functional Studies |
Use at an assay dependent concentration.
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| Notes |
|---|
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Functional Studies
Use at an assay dependent concentration. |
Images
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Chemical Structure - ICI 182,780, Estrogen receptor antagonist (ab120131)2D chemical structure image of ab120131, ICI 182,780, Estrogen receptor antagonist
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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 (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
Protocols
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
References (7)
ab120131 has been referenced in 7 publications.
- Xiao L et al. Profile of melatonin and its receptors and synthesizing enzymes in cumulus-oocyte complexes of the developing sheep antral follicle-a potential estradiol-mediated mechanism. Reprod Biol Endocrinol 17:1 (2019). PubMed: 30606208
- Traboulsi T et al. Role of SUMOylation in differential ERa transcriptional repression by tamoxifen and fulvestrant in breast cancer cells. Oncogene 38:1019-1037 (2019). PubMed: 30190545
- Xu X et al. 17ß-Estradiol nongenomically induces vascular endothelial H2S release by promoting phosphorylation of cystathionine ?-lyase. J Biol Chem 294:15577-15592 (2019). PubMed: 31439665
- Wang Z et al. The in vitro estrogenic activity of the crude drugs found in Japanese herbal medicines prescribed for menopausal syndrome was enhanced by combining them. BMC Complement Altern Med 18:107 (2018). PubMed: 29566679
- Keil KP et al. In vivo and in vitro sex differences in the dendritic morphology of developing murine hippocampal and cortical neurons. Sci Rep 7:8486 (2017). PubMed: 28814778
- Xiao L et al. Induction of the CLOCK gene by E2-ERa signaling promotes the proliferation of breast cancer cells. PLoS One 9:e95878 (2014). PubMed: 24789043
- Schennink A et al. A novel first exon directs hormone-sensitive transcription of the pig prolactin receptor. J Mol Endocrinol 51:1-13 (2013). PubMed: 23576686