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Fulvestrant

Cat. No. M1966
Fulvestrant Structure
Synonym:

Faslodex, ICI 182780

Size Price Availability Quantity
50mg USD 125 In stock
200mg USD 280 In stock
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Quality Control
Biological Activity

Fulvestrant (Faslodex) is a new estrogen receptor (ER) antagonist for the treatment of advanced breast cancer. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant is a potent inhibitor of the growth of human breast cancer cells in vitro and in vivo. It has demonstrated pure anti-estrogenic activity in animal systems. Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor. Because of a different mode of action to that of other hormonal agents, fulvestrant is effective in the treatment of tamoxifen-resistant disease and, unlike tamoxifen, has no known estrogen agonist effects.

Protocol
Cell Experiment
Cell lines MCF-7
Preparation method MCF-7 cells were plated at 10 000 cells/well in 96-well culture plates in MEM with 10% fetal bovine serum, and they were allowed to adhere for 48 h. Thereafter, the cultures were washed with serum-free MEM and incubated in 100 μl serum-free MEM. After 72 h, the medium was removed and replaced with 2% charcoal-stripped FBS–MEM containing 10 pmol/l E2 with either RAD1901 or additional E2 at concentrations ranging from 10−15 to 10−6 mol/l. The medium was removed after 48 h of incubation and the cells were lysed by adding 100 μl of CellTiter Glo (Promega, Madison, Wisconsin, USA), diluted 1 : 1 in water, per well. The plates were gently mixed on a plate shaker for 10 min before the luminescent signal was measured on a luminometer. The EC50 and IC50 of the test compound were defined as the concentrations that resulted in half-maximum shift.
Concentrations Ranging from 10−15 to 10−6 mol/l
Incubation time 48 h
Animal Experiment
Animal models MCF-7 xenograft models: Female athymic nude mice [Crl:NU(NCr)-Foxn1nu]
Formulation Formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water
Dosages 0.5 mg/animal daily
Administration subcutaneous injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 606.77
Formula C32H47F5O3S
CAS Number 129453-61-8
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Oncotarget (2016). Figure 5. ICI-182780 (Abmole Bioscience Kowloon, Hong Kong).
Method
Cell Lines CD4+CD62L+ T Cell
Concentrations 0.1 μM
Incubation Time 3 d
Results As shown in Figure 5A and 5B, neither MPP nor G15 showed noticeable effect on the decreased percentage of Th17 (IL-17A+CD4+ T) cells induced by arctigenin. Both ICI and PHTPP themselves did not affect the Th17 differentiation, but they markedly diminished the inhibitory effect of arctigenin. As expected, E2 could effectively decrease the percentage of Th17 cells. An addition of ICI also diminished the inhibitory effect of E2 on Th17 differentiation. Arctigenin markedly increased the expressions of ERβ target genes CAV1 and ENPP2, but showed no obvious effect on the expression of ERβ during Th17 differentiation (Figure 5C), which coincided well with the fact that arctigenin specifically promoted the expression of ERβ target genes in EL4 cells.
Rating
Source Breast Cancer Res Treat (2015). Figure 4.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole),
Method tumor volume, Ki67 staining, western bolt
Cell Lines T47D/FR
Concentrations 5 mg/week s.c. in 100 µL
Incubation Time 3 days(wb) or 8 weeks
Results "P7170 (in the context of a fulvestrant backbone) significantly decreased cell proliferation in T47D/FR tumors, but did not significantly increase apoptosis."
Rating
Source Breast Cancer Res Treat (2015). Figure 3.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole),
Method tumor volume, western blot, H&E staining, Ki67 staining, TUNEL test
Cell Lines MCF-7
Concentrations 5 mg/week s.c. in 100 µL
Incubation Time 3 days(wb) or 4-6 weeks
Results The addition of 5 mg/kg/day P7170 to fulvestrant significantly decreased tumor volumes compared to fulvestrant alone after 3–4.5 weeks of treatment (p<0.05)
Rating
Source Breast Cancer Res Treat (2015). Figure 2.Fulvestrant was obtained either in the clinical formulation (Astrazeneca) or in the powder form (Abmole),
Method flow cytometry
Cell Lines MCF-7, MCF-7/FR, MCF-7/LTED, HCC-1428, T47D, T47D/FR
Concentrations 1 µM
Incubation Time 3-4 days
Results In MCF-7, MCF-7/LTED, T47D, and T47D/FR cells, the combination of P7170 and fulvestrant significantly increased apoptosis compared to either drug alone.
Rating
Product Citations
References

Fulvestrant - a novel endocrine therapy for breast cancer.
Johnston SJ, et al. Curr Med Chem. 2010;17(10):902-14. PMID: 20156170.

Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: a multinational, double-blind, randomized trial.
Howell A, et al. J Clin Oncol. 2004 May 1;22(9):1605-13. PMID: 15117982.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Fulvestrant, Faslodex, ICI 182780 supplier, Estrogen Receptor, inhibitors

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