Fulvestrant (ICI 182780)

Alias: ZD9238; ICI-182780; ZM182780;ZD-9238; ICI182780; ZM 182780;ZD 9238; ICI 182780; ZM-182780; Fulvestrant; Faslodex.
Cat No.:V1721 Purity: ≥98%
Fulvestrant (ICI-182780; ZD-9238; ZM-182780;Faslodex) is a synthetic and potent estrogen receptor (ER) antagonist approved asa medication for the treatment of hormone receptor (HR)-positive breast cancer in postmenopausal women.
Fulvestrant (ICI 182780) Chemical Structure CAS No.: 129453-61-8
Product category: Estrogenprogestogen Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Fulvestrant (ICI 182780):

  • Fulvestrant S enantiomer
  • Fulvestrant R enantiomer
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Fulvestrant (ICI-182780; ZD-9238; ZM-182780; Faslodex) is a synthetic and potent estrogen receptor (ER) antagonist approved as a medication for the treatment of hormone receptor (HR)-positive breast cancer in postmenopausal women. It ihibits ER with an IC50 of 0.94 nM in a cell-free assay. Unlike tamoxifen, which has partial agonist effects, and the aromatase inhibitors, which reduce the estrogen available to tumor cells, fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
FuLvestrant (ICI 182780; ZD 9238; ZM 182780) is a very effective and selective oestrogen action inhibitor that shows superior growth suppression in animal models and human breast cancer cells. With an IC50 of 0.29 nM, fuLvestrant stops the development of MCF-7 human breast cancer cells. Fulvestrant has a relative binding affinity of 0.89. FuLvestrant maintains its pure estrogen antagonist activity while having a markedly increased antiestrogenic potency [1]. Fulvestrant, an ER antagonist that downregulates ER, is the first new class of endocrine control medication[3]. ERα expression in MCF-7 cells was not affected by 1 μM ICI 47699 treatment, while it was fully suppressed by 100 nM FuLvestrant [4].
ln Vivo
When given by itself, fulvestrant (ICI 182,780) exhibits no uterotropic activity parenterally (sc) in immature female rats. Fulvestrant completely opposes the effects of estrogen at a dose of 0.5 mg/kg/day sc. Oral fulvestrant (5 mg/kg/day) treatment and subcutaneous administration are qualitatively comparable [1]. in two human breast cancer models in naked mice. After a single injection, fulvestrant (5 mg) in one of the models totally stopped the growth of MCF-7 tumor xenografts for at least 4 weeks. Fulvestrant suppressed existing tumor growth for twice as long and delayed tumor growth more than treatment with ICI 47699 in additional experiments conducted in nude mice carrying MCF-7 xenografts. Large[3]. At day 40, fulvestrant showed 88% tumor growth inhibition (TGI) [4].
Animal Protocol
Formulated to 50 mg/mL in arachis oil; 5 mg/mouse; s.c. injection
The human breast cancer xenografts MCF-7 in nude mice
References
[1]. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73.
[2]. Yu X, et al.MiR-214 increases the sensitivity of breast cancer cells to tamoxifen and fulvestrant through inhibition of autophagy.Mol Cancer. 2015 Dec 15;14:208.
[3]. Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1:S2-6.
[4]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56
[5]. Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27(7):1700-9
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C32H47F5O3S
Molecular Weight
606.77
CAS #
129453-61-8
SMILES
C[C@@]12[C@@H](O)CC[C@@]1([H])[C@]3([H])[C@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)CC4=C(C=CC(O)=C4)[C@@]3([H])CC2
Synonyms
ZD9238; ICI-182780; ZM182780;ZD-9238; ICI182780; ZM 182780;ZD 9238; ICI 182780; ZM-182780; Fulvestrant; Faslodex.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (164.8 mM)
Water:<1 mg/mL
Ethanol: 100 mg/mL (164.8 mM)
Solubility (In Vivo)
5%DMSO+95%Corn oil: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6481 mL 8.2404 mL 16.4807 mL
5 mM 0.3296 mL 1.6481 mL 3.2961 mL
10 mM 0.1648 mL 0.8240 mL 1.6481 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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