Fulvestrant

Catalog No.S1191 Batch:S119121

Technical Data

Formula

C₃₂H₄₇F₅O₃S

Molecular Weight

606.77

CAS No.

129453-61-8

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (164.8 mM)

Ethanol

100 mg/mL (164.8 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O

0.4mg/ml

Taking the 1 mL working solution as an example, add 20 μL of clarified DMSO stock solution of 20 mg/ml to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

Targets

ER ^[1]
(Cell-free assay)

0.94 nM

In vitro

Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. ^[1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. ^[2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. ^[3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. ^[4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. ^[5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. ^[6]

In vivo

Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant. ^[1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. ^[7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. ^[8]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MCF-7 breast cancer cells Concentrations 2.9 nM Incubation Time 5 days Method MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 10⁴) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.
Animal Study:^{^[6]}	Animal Models The human breast cancer xenografts MCF-7 in nude mice Dosages 5 mg/mouse Administration s.c. injection

Cell Assay:^{^[1]}

Cell lines
MCF-7 breast cancer cells
Concentrations
2.9 nM
Incubation Time
5 days
Method
MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 10⁴) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.

Animal Study:^{^[6]}

Animal Models
The human breast cancer xenografts MCF-7 in nude mice
Dosages
5 mg/mouse
Administration
s.c. injection

References

+ Expand

Customer Product Validation

: Data from [Data independently produced by Mol Cancer Ther, 2014, 13(1), 230-8]

: Data from [PLoS One, 2011, 6, e21112]

: Data from [PLoS One, 2011, 6, e21112]

: , , Oncogene, 2017, 36(16):2255-2264

Selleck's Fulvestrant has been cited by 161 publications

Macrophages Promote Subtype Conversion and Endocrine Resistance in Breast Cancer [ Cancers (Basel), 2024, 16(3)678]	PubMed: 38339428
Testing Adaptive Therapy Protocols Using Gemcitabine and Capecitabine in a Preclinical Model of Endocrine-Resistant Breast Cancer [ Cancers (Basel), 2024, 16(2)257]	PubMed: 38254748
Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899]	PubMed: none
Novel Estrogen Receptor Dimerization BRET-Based Biosensors for Screening Estrogenic Endocrine-Disrupting Chemicals [ Biomater Res, 2024, 28:0010]	PubMed: 38464469
Short-term tamoxifen administration improves hepatic steatosis and glucose intolerance through JNK/MAPK in mice [ Signal Transduct Target Ther, 2023, 8(1):94]	PubMed: 36864030
Cell facilitation promotes growth and survival under drug pressure in breast cancer [ Nat Commun, 2023, 14(1):3851]	PubMed: 37386030
N-acetylcysteine overcomes NF1 loss-driven resistance to PI3Kα inhibition in breast cancer [ Cell Rep Med, 2023, 4(4):101002]	PubMed: 37044095
Co-targeting RANK pathway treats and prevents acquired resistance to CDK4/6 inhibitors in luminal breast cancer [ Cell Rep Med, 2023, 4(8):101120]	PubMed: 37451269
Co-targeting RANK pathway treats and prevents acquired resistance to CDK4/6 inhibitors in luminal breast cancer [ Cell Rep Med, 2023, 4(8):101120]	PubMed: 37451269
CCNE1 and PLK1 Mediate Resistance to Palbociclib in HR+/HER2- Metastatic Breast Cancer [ Clin Cancer Res, 2023, 29(8):1557-1568]	PubMed: 36749874

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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