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Fulvestrant

Cat. No. M1966
Fulvestrant Structure
Synonym:

ICI 182780; ZD 9238; ZM 182780

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
10mg USD 45  USD45 In stock
50mg USD 140  USD140 In stock
100mg USD 260  USD260 In stock
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Quality Control & Documentation
Biological Activity

Fulvestrant is a Estrogen receptor (ER) antagonist with IC50 of 0.094 nM. Fulvestrant effectively inhibited the growth of ER-positive McF-7 (IC50 = 0.29 nM), but had no effect on the growth of Er-negative BT-20 human breast cancer cells. Fulvestrant causes cells to accumulate in the G0/G1 phase and also reduces the proportion of cells capable of continuous DNA synthesis. Fulvestrant competitively inhibits estradiol binding to estrogen receptors. Fulvestrant can also induce autophagy and apoptosis, and has anti-tumor effect.

Product Citations
Customer Product Validations & Biological Datas
Source Int J Biol Sci (2018 Oct). Figure 6. Fulvestrant (Abmole Bioscience, Houston, USA)
Method subcutaneously
Cell Lines Conditional Brca1-knockout and MMTV-Cre transgenic mice
Concentrations 250 mg/kg
Incubation Time -
Results The chemotherapeutic efficacy of fulvestrant was examined in 18 sets of allograft mice produced from tumors from 18 individuals.
Source Int J Biol Sci (2018 Oct). Figure 5. Fulvestrant (Abmole Bioscience, Houston, USA)
Method subcutaneously
Cell Lines Conditional Brca1-knockout and MMTV-Cre transgenic mice
Concentrations 250 mg/kg
Incubation Time -
Results In addition, histological analyses revealed that the number and size of lobular and ductal tubes were reduced in fulvestrant-treated mammary glands and their structure showed evidence of degeneration and shrinkage.
Source Int J Biol Sci (2018 Oct). Figure 4. Fulvestrant (Abmole Bioscience, Houston, USA)
Method subcutaneously
Cell Lines Conditional Brca1-knockout and MMTV-Cre transgenic mice
Concentrations 250 mg/kg
Incubation Time -
Results In addition, fulvestrant-treated tumors displayed large necrotic areas with a lower level of the proliferation marker, and higher levels of cleaved caspase-3 and positive TUNEL staining compared with untreated tumor tissues (Fig. 4C), suggesting that estrogen signaling contributes to altered aggressiveness of Brca1-mutant tumors.
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.
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."
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)
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 606.77
Formula C32H47F5O3S
CAS Number 129453-61-8
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Johnston SJ, et al. Curr Med Chem. Fulvestrant - a novel endocrine therapy for breast cancer.

[2] Howell A, et al. J Clin Oncol. 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.

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Keywords: Fulvestrant, ICI 182780; ZD 9238; ZM 182780 supplier, Estrogen Receptor, inhibitors, activators


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