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ICI 182,780 (Fulvestrant)

(HB2501)
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Product overview

Name ICI 182,780 (Fulvestrant)
Alternative names Fulvestrant
Purity >99%
Description Estrogen receptor (ER) antagonist and high affinity GPER agonist
Biological Data Solubility & Handling Chemical Data Related Areas Calculators Technical guides (1) Reviews References (4) Frequently bought together
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Biological Data

Biological description Estrogen receptor (ER) antagonist (Ki values are 1 and 3.6 nM at ERα and ERβ respectively). Shows no agonist activity and is devoid of estrogenic activity. Also a high affinity agonist at GPER (GPR30). Down-regulates the ER and impairs nuclear shuttling and dimerization of the receptor. Shows anticancer activity. Active in vivo.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100 mM), and in ethanol (50 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

Molarity

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Dilution

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Chemical Data

Purity >99%
Chemical name 7α,17β-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
Molecular Weight 606.77
Chemical structure ICI 182,780 Chemical Structure
Molecular Formula C32H47F5O3S
CAS Number 129453-61-8
PubChem identifier 104741
SMILES C[C@]12CC[C@H]3[C@H]([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
MDL number MFCD00903953
Appearance White solid

References for ICI 182,780 (Fulvestrant)

References are publications that support the biological activity of the product

  • Emerging data on the efficacy and safety of fulvestrant, a unique antiestrogen therapy for advanced breast cancer.

    Scott SM et al (2011) Expert Opin Drug Saf 10(5) : 819-26.
    Read more (PubMedID: 21699443)

  • Estrogen and its receptors in cancer.

    Chen GG et al (2008) Med Res Rev 28(6) : 954-74.
    Read more (PubMedID: 18642351)

  • Antagonists selective for estrogen receptor alpha.

    Sun J et al (2002) Endocrinology 143(3) : 941-7.
    Read more (PubMedID: 11861516)

  • Activation of the human estrogen receptor by the antiestrogens ICI 182,780 and tamoxifen in yeast genetic systems: implications for their mechanism of action.

    Dudley MW et al (2000) Proc Natl Acad Sci U S A 97(7) : 3696-701.
    Read more (PubMedID: 10725345)

4 Item(s)

Related Products
Grouped product items
Order: HB2501
Pack PriceQty
1mg
$63
10mg
$107
50mg
$248
Estrogen receptor (ER) antagonist and high affinity GPER agonist
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