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ICI 182,780 (CAS 129453-61-8)

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Alternate Names:
Fulvestrant; Faslodex
Application:
ICI 182,780 is an estrogen receptor inhibitor and GPR30 activator
CAS Number:
129453-61-8
Purity:
≥98%
Molecular Weight:
606.77
Molecular Formula:
C32H47F5O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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ICI 182,780 is a high affinity estrogen receptor antagonist (IC50 = 0.29 nM), devoid of any partial agonism in vitro and ICI 182,780 is also a high affinity agonist at the membrane estrogen receptor, GPR30. ICI 182, 780, has various biochemical and physiological effects on the body. It reduces circulating estradiol levels, which is the primary form of estrogen in the body. Moreover, it inhibits the expression of genes related to cell proliferation, angiogenesis, migration, and invasion. It also has anti-inflammatory and anti-oxidant effects.


ICI 182,780 (CAS 129453-61-8) References

  1. Insulin receptor substrate 1 is a target for the pure antiestrogen ICI 182,780 in breast cancer cells.  |  Salerno, M., et al. 1999. Int J Cancer. 81: 299-304. PMID: 10188734
  2. 17beta-estradiol and ICI-182780 regulate the hair follicle cycle in mice through an estrogen receptor-alpha pathway.  |  Chanda, S., et al. 2000. Am J Physiol Endocrinol Metab. 278: E202-10. PMID: 10662703
  3. ICI 182,780 (Faslodex): development of a novel, 'pure' antiestrogen.  |  Howell, A., et al. 2000. Cancer. 89: 817-25. PMID: 10951345
  4. Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex).  |  McClelland, RA., et al. 2001. Endocrinology. 142: 2776-88. PMID: 11415996
  5. The antiestrogen ICI 182,780 induces early effects on the adult male mouse reproductive tract and long-term decreased fertility without testicular atrophy.  |  Cho, HW., et al. 2003. Reprod Biol Endocrinol. 1: 57. PMID: 12959643
  6. The antiestrogen ICI 182,780 decreases the expression of estrogen receptor-alpha but has no effect on estrogen receptor-beta and androgen receptor in rat efferent ductules.  |  Oliveira, CA., et al. 2003. Reprod Biol Endocrinol. 1: 75. PMID: 14613549
  7. Antiuterotrophic effects of a pure antioestrogen, ICI 182,780: magnetic resonance imaging of the uterus in ovariectomized monkeys.  |  Dukes, M., et al. 1992. J Endocrinol. 135: 239-47. PMID: 1474330
  8. Leptin interferes with the effects of the antiestrogen ICI 182,780 in MCF-7 breast cancer cells.  |  Garofalo, C., et al. 2004. Clin Cancer Res. 10: 6466-75. PMID: 15475434
  9. Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.  |  Thomas, P., et al. 2005. Endocrinology. 146: 624-32. PMID: 15539556
  10. P-cadherin is up-regulated by the antiestrogen ICI 182,780 and promotes invasion of human breast cancer cells.  |  Paredes, J., et al. 2004. Cancer Res. 64: 8309-17. PMID: 15548699
  11. Fulvestrant (ICI 182,780)-dependent interacting proteins mediate immobilization and degradation of estrogen receptor-alpha.  |  Long, X. and Nephew, KP. 2006. J Biol Chem. 281: 9607-15. PMID: 16459337
  12. A potent specific pure antiestrogen with clinical potential.  |  Wakeling, AE., et al. 1991. Cancer Res. 51: 3867-73. PMID: 1855205
  13. The estrogen antagonist ICI 182,780 reduces cancellous bone volume in female rats.  |  Gallagher, A., et al. 1993. Endocrinology. 133: 2787-91. PMID: 8243306
  14. ICI 182,780: a pure antiestrogen that affects behaviors and energy balance in rats without acting in the brain.  |  Wade, GN., et al. 1993. Am J Physiol. 265: R1392-8. PMID: 8285282
  15. Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting oestradiol- and IGF-I-induced proliferation of human breast cancer-derived cells.  |  de Cupis, A., et al. 1995. Br J Pharmacol. 116: 2391-400. PMID: 8581274

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

ICI 182,780, 1 mg

sc-203435
1 mg
$81.00

ICI 182,780, 10 mg

sc-203435A
10 mg
$183.00

Hi, Wondering if the stock solution in DMSO should be kept in -20 or RT? Thanks

Asked by: Azadeh
Thank you for your question. We recommend storing for up to 6 months at -20-80℃ in solvent.
Answered by: Technical Support
Date published: 2017-10-31

What is the stability of the compound after reconstitution with water?

Asked by: two2igm05
Thank you for your question. ICI 182,780, sc-203435, can be stored for 3 years at -20℃ as a powder or for 6 months at -80℃ in solvent.
Answered by: TechService7
Date published: 2017-01-16
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Rated 5 out of 5 by from YiYi, JH. et al. (PubMed 25534230) used ICI 182,780 (Fulvestrant), a high affinity estrogen receptor antagonist, to investigate the role of the estrogen receptor (ER) in gastric cancer cell lines positive for ER- . When ERs were inhibited by ICI 182,780 gastric cancer cell proliferation was suppressed. -SCBT Publication Review
Date published: 2015-06-02
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ICI 182,780 is rated 5.0 out of 5 by 1.
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