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MedKoo product information:
Fulvestrant
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MedKoo Code#: 100390
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Name:
Fulvestrant
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CAS#: 129453-61-8
Synonym: US
brand name: Faslodex. Code names: ICI 182,780; ZD9238. Chemical
structure name: 7a-[9-[(4,4,5,5,5,-Pentafluoropentyl)sulphinyl]nonyl]-estra-1,3,5(10)-triene-3,17b-diol;
7-alpha-[9-(4,4,5,5,5-penta fluoropentylsulphinyl) nonyl]estra-1,3,5-(10)-
triene-3,17-beta-diol
IUPAC/Chemical name:
(7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
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Chemical structure:
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Theoretical analysis
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Chemical Formula: C32H47F5O3S
Exact Mass: 606.31661
Molecular Weight: 606.77
m/z: 606.31661 (100.0%), 607.31996 (34.6%),
608.32332 (5.8%), 608.31240 (4.5%), 609.31576 (1.6%)
Elemental Analysis: C, 63.34; H, 7.81; F,
15.66; O, 7.91; S, 5.28
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Availability and price:
This agent is
available through our partner. For quotation, question, and order, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer significant discount
for larger quantity order.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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Fulvestrant is a synthetic estrogen receptor antagonist. 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. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus)
Fulvestrant is a white powder with a molecular weight of 606.77. The
solution for injection is a clear, colorless to yellow, viscous
liquid. Each injection contains as inactive ingredients: Alcohol,
USP, Benzyl Alcohol, NF, and Benzyl Benzoate, USP, as co-solvents,
and Castor Oil, USP as a co-solvent and release rate modifier.
FASLODEX is supplied in sterile single patient pre-filled syringes
containing 50-mg/mL fulvestrant either as a single 5 mL or two
concurrent 2.5 mL injections to deliver the required monthly dose.
FASLODEX is administered as an intramuscular injection of 250 mg
once monthly.
Many
breast cancers have estrogen receptors (ER), and the growth of these
tumors can be stimulated by estrogen. Fulvestrant is an estrogen
receptor antagonist that binds to the estrogen receptor in a competitive
manner with affinity comparable to that of estradiol. Fulvestrant
downregulates the ER protein in human breast cancer cells.
In a clinical study in postmenopausal women with primary breast cancer
treated with single doses of FASLODEX 15-22 days prior to surgery, there
was evidence of increasing down regulation of ER with increasing dose.
This was associated with a dose-related decrease in the expression of
the progesterone receptor, an estrogen-regulated protein. These effects
on the ER pathway were also associated with a decrease in Ki67 labeling
index, a marker of cell proliferation.
In vitro studies demonstrated that fulvestrant is a reversible inhibitor
of the growth of tamoxifen-resistant, as well as estrogen-sensitive
human breast cancer (MCF-7) cell lines. In in vivo tumor studies,
fulvestrant delayed the establishment of tumors from xenografts of human
breast cancer MCF-7 cells in nude mice. Fulvestrant inhibited the growth
of established MCF-7 xenografts and of tamoxifen-resistant breast tumor
xenografts. Fulvestrant resistant breast tumor xenografts may also be
cross-resistant to tamoxifen.
Fulvestrant showed no agonist-type effects in in vivo uterotropic assays
in immature or ovariectomized mice and rats. In in vivo studies in
immature rats and ovariectomized monkeys, fulvestrant blocked the
uterotrophic action of estradiol. In postmenopausal women, the absence
of changes in plasma concentrations of FSH and LH in response to
fulvestrant treatment (250 mg monthly) suggests no peripheral steroidal
effects.
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1129: Arao Y, Kikuchi A, Ikeda K, Nomoto S, Horiguchi H, Kayama F.
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