Cat. No.: HY-13636

Fulvestrant

(Synonyms: ICI 182780; ZD 9238; ZM 182780)

139 Cited Publications

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Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

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Pureté: 99.98%
CAS No.: 129453-61-8
Formule: C₃₂H₄₇F₅O₃S
Masse moléculaire:606.77

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fulvestrant Chemical Structure

CAS No.: 129453-61-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (139)
Solvant et solubilité
- In Vitro
- In Vivo
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Activité biologique

Description

IC₅₀ & Target

IC50: 9.4 nM (Estrogen Receptor)^[1]

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR :

Cellular Effect

Cell Line	Type	Value	Description	References
Cancer cell lines	IC₅₀	0.004 μM Compound: Fulvestrant, ICI-182780	Inhibition of 10e-9 M E2 stimulated MCF-7 breast cancer cell proliferation Inhibition of 10e-9 M E2 stimulated MCF-7 breast cancer cell proliferation	[PMID: 15324884]
Cancer cell lines	IC₅₀	0.005 μM Compound: Fulvestrant, ICI-182780	Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cells Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cells	[PMID: 15324884]
Cancer cell lines	IC₅₀	0.21 nM Compound: Fulvestrant, ICI-182780	Inhibition of ER-MDA-MB 231 breast cancer cell proliferation over 200 hr Inhibition of ER-MDA-MB 231 breast cancer cell proliferation over 200 hr	[PMID: 15324884]
COS-7	IC₅₀	3.8 nM Compound: Fulvestrant	Antagonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay Antagonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	[PMID: 19863083]
COS-7	IC₅₀	4 nM Compound: Fulvestrant	Antagonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay Antagonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	[PMID: 19863083]
COS-7	IC₅₀	34 μM Compound: Fulvestrant	Cytotoxicity against African green monkey COS7 cells assessed as reduction in cell mass measured after 72 hrs by crystal violet staining based assay Cytotoxicity against African green monkey COS7 cells assessed as reduction in cell mass measured after 72 hrs by crystal violet staining based assay	[PMID: 32169784]
HEK293	EC₅₀	1.4 nM Compound: Fulvestrant	Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay	[PMID: 30940565]
HEK293	IC₅₀	0.78 nM Compound: Fulvestrant	Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay	[PMID: 30940565]
HepG2	EC₅₀	1.95 μM Compound: 3	Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay	[PMID: 23688559]
LNCaP	IC₅₀	18 nM Compound: ICI-182780, Fulvestrant	Cytotoxicity against human LNCAP cells after 4 days by MTT assay Cytotoxicity against human LNCAP cells after 4 days by MTT assay	[PMID: 19467602]
MCF-10A	IC₅₀	>100 μM Compound: 3; FUL	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF-10A	IC₅₀	>100 μM Compound: Ful	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MCF-10A	IC₅₀	>100 μM Compound: 4; Ful	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
MCF-10A	IC₅₀	>100 μM Compound: Ful	Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	0.47 nM Compound: 2, ICI-182780	Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha	[PMID: 10673099]
MCF7	IC₅₀	18 nM Compound: ICI-182780, Fulvestrant	Cytotoxicity against human MCF7 cells after 4 days by MTT assay Cytotoxicity against human MCF7 cells after 4 days by MTT assay	[PMID: 19467602]
MCF7	IC₅₀	2 nM Compound: ICI-182,780	Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method	[PMID: 23448346]
MCF7	IC₅₀	1.9 nM Compound: ICI 182780	Inhibition of 17beta-estradiol-induced in ERalpha positive human MCF7 cells proliferation assessed as [3H]-thymidine incorporation after 72 hrs by liquid scintillation counting Inhibition of 17beta-estradiol-induced in ERalpha positive human MCF7 cells proliferation assessed as [3H]-thymidine incorporation after 72 hrs by liquid scintillation counting	[PMID: 24908652]
MCF7	IC₅₀	0.6 nM Compound: 3	Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay	[PMID: 25879485]
MCF7	IC₅₀	0.6 μM Compound: 3	Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay	[PMID: 25879485]
MCF7	EC₅₀	0.0004 μM Compound: 3	Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 25879485]
MCF7	EC₅₀	0.4 nM Compound: 3	Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 25879485]
MCF7	EC₅₀	0.4 nM Compound: 1	Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay	[PMID: 26463130]
MCF7	IC₅₀	0.6 nM Compound: 1	Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay	[PMID: 26463130]
MCF7	IC₅₀	0.0015 μM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
MCF7	IC₅₀	0.044 μM Compound: Fulvestrant	Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
MCF7	IC₅₀	4.4 nM Compound: 5	Antiproliferative activity against human MCF7 cells after 6 days in presence of estradiol by CellTiter-Glo assay Antiproliferative activity against human MCF7 cells after 6 days in presence of estradiol by CellTiter-Glo assay	[PMID: 29562737]
MCF7	IC₅₀	<0.1 nM Compound: 1	Antiproliferative activity against human MCF7 cells after 6 days by WST-1 assay Antiproliferative activity against human MCF7 cells after 6 days by WST-1 assay	[PMID: 30128071]
MCF7	EC₅₀	0.4 nM Compound: Fulvestrant	Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay	[PMID: 30587451]
MCF7	IC₅₀	0.6 nM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay	[PMID: 30587451]
MCF7	GI₅₀	0.17 nM Compound: 5	Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis	[PMID: 30990042]
MCF7	IC₅₀	4.93 μM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells assessed as reduction in cell mass measured after 72 hrs by crystal violet staining based assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell mass measured after 72 hrs by crystal violet staining based assay	[PMID: 32169784]
MCF7	IC₅₀	0.32 nM Compound: 1	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis	[PMID: 32551022]
MCF7	IC₅₀	2.6 nM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay	[PMID: 32551022]
MCF7	IC₅₀	0.35 nM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 33138369]
MCF7	IC₅₀	0.58 nM Compound: Fulvestrant	Antiproliferative activity against human ER-positive MCF7 cells assessed as reduction in cell viability measured after 120 hrs by crystal violet staining based assay Antiproliferative activity against human ER-positive MCF7 cells assessed as reduction in cell viability measured after 120 hrs by crystal violet staining based assay	[PMID: 33904307]
MCF7	EC₅₀	2.4 nM Compound: 1	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay	[PMID: 34251202]
MCF7	GI₅₀	0.54 μM Compound: Ful	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 6 days by WST8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 6 days by WST8 assay	[PMID: 34610548]
MCF7	IC₅₀	0.29 nM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth	[PMID: 35964426]
MCF7	IC₅₀	0.1 nM Compound: 3	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	[PMID: 37019030]
MCF7	IC₅₀	0.16 μM Compound: 3; FUL	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF7	IC₅₀	0.33 μM Compound: Ful	Antiproliferative activity against human tamoxifen-sensitive MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human tamoxifen-sensitive MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MCF7	EC₅₀	21 nM Compound: 1	Anti-proliferative activity against wild type human MCF7 cells assessed as reduction in cell growth by CellTiter-Glo assay Anti-proliferative activity against wild type human MCF7 cells assessed as reduction in cell growth by CellTiter-Glo assay	[PMID: 37377342]
MCF7	EC₅₀	262 nM Compound: 1	Anti-proliferative activity against human MCF7 cells harboring ERalpha Y537S mutant assessed as reduction in cell growth by CellTiter-Glo assay Anti-proliferative activity against human MCF7 cells harboring ERalpha Y537S mutant assessed as reduction in cell growth by CellTiter-Glo assay	[PMID: 37377342]
MCF7	EC₅₀	265 nM Compound: 1	Anti-proliferative activity against human MCF7 cells harboring ERalpha D538G mutant assessed as reduction in cell growth by CellTiter-Glo assay Anti-proliferative activity against human MCF7 cells harboring ERalpha D538G mutant assessed as reduction in cell growth by CellTiter-Glo assay	[PMID: 37377342]
MCF7	IC₅₀	0.12 μM Compound: 4; Ful	Antiproliferative activity against ERalpha positive human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha positive human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
MCF7	IC₅₀	0.7 nM Compound: Fulvestrant	Antiproliferative activity against wildtype human MCF7 cells assessed as inhibition of cell proliferation incubated for 6 days in presence of beta-estradiol by CellTiter-Glo assay Antiproliferative activity against wildtype human MCF7 cells assessed as inhibition of cell proliferation incubated for 6 days in presence of beta-estradiol by CellTiter-Glo assay	[PMID: 38007911]
MCF7	IC₅₀	0.16 μM Compound: Ful	Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	0.61 μM Compound: Ful	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	0.62 μM Compound: Ful	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	1.2 μM Compound: Ful	Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	6.46 x 10^-4 μM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells incubated for 5 days by MTT assay Antiproliferative activity against human MCF7 cells incubated for 5 days by MTT assay	[PMID: 38870830]
MCF7	IC₅₀	0.49 nM Compound: 3, ICI-182780	Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells	[PMID: 9154963]
MCF-7/TAMR-1	IC₅₀	1.8 nM Compound: Fulvestrant	Antiproliferative activity against human MCF-7/TAMR-1 cells assessed as reduction in cell viability measured after 120 hrs by crystal violet staining based assayy Antiproliferative activity against human MCF-7/TAMR-1 cells assessed as reduction in cell viability measured after 120 hrs by crystal violet staining based assayy	[PMID: 33904307]
MDA-MB-231	IC₅₀	196.3 μM Compound: Fulvestrant	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	>100 μM Compound: Ful	Antiproliferative activity against triple negative human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against triple negative human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MDA-MB-231	IC₅₀	>100 μM Compound: 4; Ful	Antiproliferative activity against ERalpha negative human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha negative human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	0.0012 μM Compound: Fulvestrant	Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	0.042 μM Compound: Fulvestrant	Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	8.5 nM Compound: Fulvestrant	Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis	[PMID: 27529700]
T47D	IC₅₀	9.3 nM Compound: Fulvestrant	Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis	[PMID: 27529700]
T47D	IC₅₀	0.84 nM Compound: 1	Induction of ERalpha degradation in human T47D cells Induction of ERalpha degradation in human T47D cells	[PMID: 32551022]
T47D	IC₅₀	3 nM Compound: 1	Antiproliferative activity against human T47D cells assessed as reduction in cell viability Antiproliferative activity against human T47D cells assessed as reduction in cell viability	[PMID: 32551022]
T47D	IC₅₀	1.76 μM Compound: Ful	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
T47D	IC₅₀	2.21 μM Compound: Ful	Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
T47D	IC₅₀	3.92 μM Compound: Ful	Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
T47D	IC₅₀	1.76 μM Compound: 4; Ful	Antiproliferative activity against ERalpha positive human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha positive human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	2.21 μM Compound: 4; Ful	Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	3.92 μM Compound: 4; Ful	Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	2.21 nM Compound: Fulvestrant	Antiproliferative activity against human T47D cells transfected with wildtype ESR1 assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells transfected with wildtype ESR1 assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay	[PMID: 38007911]
T47D	IC₅₀	2.3 nM Compound: Fulvestrant	Antiproliferative activity against human T47D cells assessed as inhibition of proliferation incubated for 6 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells assessed as inhibition of proliferation incubated for 6 days by CellTiter-Glo assay	[PMID: 38007911]
T47D	IC₅₀	5.94 nM Compound: Fulvestrant	Antiproliferative activity against human T47D cells transfected with ESR1 Y537S mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells transfected with ESR1 Y537S mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay	[PMID: 38007911]
T47D	IC₅₀	58.57 nM Compound: Fulvestrant	Antiproliferative activity against human T47D cells transfected with ESR1 D538G mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells transfected with ESR1 D538G mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay	[PMID: 38007911]

In Vitro

Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with the IC₅₀ of 0.29 nM. The relative binding affinities of Fulvestrant is 0.89. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity^[1]. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER^[3]. Treatment of MCF-7 cells with 1 μM ICI 47699 has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

When administered alone, parenterally (s.c.), Fulvestrant (ICI 182,780) is devoid of uterotropic activity in immature female rats.
Fulvestrant (0.5 mg/kg/day s.c) shows complete antagonism of Estrogen action.
Fulvestrant by po administration (5 mg/kg/day p.o.) is qualitatively similar with s.c.^[1].
In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumor growth is delayed to a greater extent than is observed with ICI 47699 treatment^[3].
Fulvestrant exhibits tumor growth inhibition (TGI) on day 40 of 88%^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 129453-61-8
Appearance Solid
Masse moléculaire 606.77
Formule C₃₂H₄₇F₅O₃S
Color White to off-white
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

ICI 182780; ZD 9238; ZM 182780
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (139)

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Cancer Cell

Neurofibromin Is an Estrogen Receptor-α Transcriptional Co-repressor in Breast Cancer. [Abstract]

2020 Mar 16;37(3):387-402.e7. PMID: 32142667

Fulvestrant purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]

MCF-7 cells were seeded in 10^-11 M E2 to which Fulvestrant (F), Dabrafenib (D), Trametinib (T) or Selumetinib (S) were subsequently added at 10^-9, 10^-6, 10^-7 or 10^-6 M, respectively. After 6 days, proteins were measured by immunoblotting, and phosphorylation levels (as defined by the levels of the phosphorylated form over total protein) relative to the vehicle-treated cells were set to 1.

Fulvestrant purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]

Top: cells were grown for 6 days in the presence of 10^-11 M E2 and 10^-9 M Fulvestrant, to which increasing concentration of Selumetinib was added. Cell numbers relative to the vehicle control are plotted. Bottom: the cells were treated similarly except 10^-6 M Selumetinib was used, and apoptosis was measured 6 days post-treatment.
Cell

Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]

2025 May 29;188(11):3065-3080.e21. PMID: 40393457
Nat Genet

MYC activity at enhancers drives prognostic transcriptional programs through an epigenetic switch. [Abstract]

2024 Apr;56(4):663-674. PMID: 38454021

Fulvestrant purchased from MedChemExpress. Usage Cited in: Nat Genet. 2024 Apr;56(4):663-674. [Abstract]

Protein expression of ER and MYC during 1 h Fulvestrant treatment (100 nM) in MCF7 cells.
Adv Mater

Ionizable Drugs Enable Intracellular Delivery of Co-Formulated siRNA. [Abstract]

2024 Aug 15:e2403701. PMID: 39148215
Sci Bull

Nuclear receptor ESRRA promotes ERα-positive breast cancer through dual action on super enhancers and promoters to regulate gene transcriptional programs. [Abstract]

2025 Sep 29:S2095-9273(25)00984-3. PMID: 41111053

Fulvestrant purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Sep 29:S2095-9273(25)00984-3. [Abstract]

MCF7 cells were incubated in stripping medium for 3 d and were pre-treated with Fulvestrant (10 µM, 0.5 h) followed by ChIP with anti-ESRRA specific antibody.
Nat Commun

CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]

2026 Jan 22;17(1):619. PMID: 41571637
Nat Commun

Harnessing artificial intelligence to identify Bufalin as a molecular glue degrader of estrogen receptor alpha. [Abstract]

2025 Aug 22;16(1):7854. PMID: 40846852

Fulvestrant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 22;16(1):7854. [Abstract]

The colony formation assay was used to measure LCC2 cell proliferation after treatment with Bufalin or Fulvestrant (0-200 nM).

Fulvestrant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 22;16(1):7854. [Abstract]

Fulvestrant (2.0 mg/kg). Representative IHC images for detecting Ki67 expression in the tumor specimens.
Nat Commun

Regulation of enzymatic lipid peroxidation in osteoblasts protects against postmenopausal osteoporosis. [Abstract]

2025 Jan 17;16(1):758. PMID: 39824794
Sci Transl Med

Dual PI3K/mTOR inhibition is required to combat resistance to CDK4/6 inhibitor and endocrine therapy in PIK3CA-mutant breast cancer. [Abstract]

2025 Dec 17;17(829):eadp5088. PMID: 41406241

Fulvestrant purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

Fulvestrant purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

Fulvestrant purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.
Acta Pharm Sin B

Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ER α to inhibit RANKL signaling. [Abstract]

2021 Feb;11(2):442-455. PMID: 33643823
Adv Sci (Weinh)

Synthetic Ionizable Colloidal Drug Aggregates Enable Endosomal Disruption. [Abstract]

2023 May;10(13):e2300311. PMID: 36905240
Nat Chem Biol

Plasma membrane-associated ARAF condensates fuel RAS-related cancer drug resistance. [Abstract]

2025 Aug;21(8):1226-1237. PMID: 39870764
Nucleic Acids Res

An H3K4me3 reader, BAP18 as an adaptor of COMPASS-like core subunits co-activates ERα action and associates with the sensitivity of antiestrogen in breast cancer. [Abstract]

2020 Nov 4;48(19):10768-10784. PMID: 32986841
J Exp Clin Cancer Res

PARP-1 as a novel target in endocrine-resistant breast cancer. [Abstract]

2025 Jun 16;44(1):175. PMID: 40518539
J Exp Clin Cancer Res

Estrogen receptor β inhibits breast cancer cells migration and invasion through CLDN6-mediated autophagy. [Abstract]

2019 Aug 14;38(1):354. PMID: 31412908
Sci Adv

Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles. [Abstract]

2026 Jun 12;12(24):eaed2731. PMID: 42284421
J Hazard Mater

Multiple nuclear receptor-regulated endocrine disrupting effects: A case study for bisphenol-induced crosstalk between RARα and ERα signaling pathways. [Abstract]

2025 Jun 20:495:139005. PMID: 40561951
J Hazard Mater

Estrogenic and anti-estrogenic assessment of the flame retardant, 2-ethylhexyl diphenyl phosphate (EHDPP), and its metabolites: Evidence from in vitro, in silico, and transcriptome studies. [Abstract]

2025 Jan 20:488:137303. PMID: 39862785
Environ Sci Technol

Angiogenic Activity and Mechanism for Bisphenols on Endothelial Cell and Mouse: Evidence of a Structural-Selective Effect. [Abstract]

2023 Aug 15;57(32):11803-11813. PMID: 37505069
Int J Biol Sci

Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]

2019 Jan 1;15(3):522-532. PMID: 30745839
Environ Health Perspect

Combined Effects of Polystyrene Nanosphere and Homosolate Exposures on Estrogenic End Points in MCF-7 Cells and Zebrafish. [Abstract]

2024 Feb;132(2):27011. PMID: 38381479
Genome Biol

Endometrial tumorigenesis involves epigenetic plasticity demarcating non-coding somatic mutations and 3D-genome alterations. [Abstract]

2025 May 9;26(1):124. PMID: 40346709
Proc Natl Acad Sci U S A

Evaluation of targeted and immune combination therapies in a rat model of hormone receptor-positive breast cancer. [Abstract]

2026 Feb 10;123(6):e2501052123. PMID: 41642991
Int J Biol Macromol

Estrogen receptor β mediates the feedback loop between 17β-Estradiol and CYP19A1, which controls transcriptomic stability, inhibits granulosa cell apoptosis, induces oocyte maturation and influences sow fertility. [Abstract]

2025 Jun;317(Pt 2):144879. PMID: 40466836
Int J Biol Macromol

Estrogen and glucocorticoid promote the lactoferrin synthesis and secretion ability of bovine mammary epithelial cells through ER and GR signaling pathways. [Abstract]

2025 Feb 2:140636. PMID: 39904446
Phytomedicine

Effects and mechanisms of frehmaglutin D and rehmaionoside C improve LPS-induced acute kidney injury through the estrogen receptor-mediated TLR4 pathway in vivo and in vitro. [Abstract]

2024 Jan:123:155218. PMID: 37980806
Free Radic Biol Med

17β-estradiol plays the anti-osteoporosis role via a novel ESR1-Keap1-Nrf2 axis-mediated stress response activation and Tmem119 upregulation. [Abstract]

2023 Feb 1:195:231-244. PMID: 36592659
NPJ Precis Oncol

Co-clinical trial targeting ER, FGFR and CDK4/6 in resistant hormone-positive breast cancer with FGFR alterations. [Abstract]

2025 Nov 7;9(1):343. PMID: 41203797
NPJ Breast Cancer

CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]

2025 Dec 3;11(1):135. PMID: 41339342
NPJ Breast Cancer

Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries. [Abstract]

2025 Nov 12;11(1):125. PMID: 41224743
NPJ Breast Cancer

Estrogen receptor inhibition mediates radiosensitization of ER-positive breast cancer models. [Abstract]

2022 Mar 10;8(1):31. PMID: 35273179
Biomed Pharmacother

The nephroprotective effects and mechanisms of rehmapicrogenin include ROS inhibition via an oestrogen-like pathway both in vivo and in vitro. [Abstract]

2021 Jun:138:111305. PMID: 33820633
Biomed Pharmacother

Estradiol promotes trophoblast viability and invasion by activating SGK1. [Abstract]

2019 Sep:117:109092. PMID: 31203134
Environ Pollut

ERα-mediated endoplasmic reticulum stress drives 4-tert-octylphenol-induced cardiac developmental toxicity in zebrafish. [Abstract]

2026 Apr 15:395:127832. PMID: 41713771
Oncogene

A bi-steric mTORC1-selective inhibitor overcomes drug resistance in breast cancer. [Abstract]

2023 Jul;42(28):2207-2217. PMID: 37264081
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Enhancer RNAs Mediate Estrogen-Induced Decommissioning of Selective Enhancers by Recruiting ERα and Its Cofactor. [Abstract]

2020 Jun 23;31(12):107803. PMID: 32579929
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The Lineage Determining Factor GRHL2 Collaborates with FOXA1 to Establish a Targetable Pathway in Endocrine Therapy-Resistant Breast Cancer. [Abstract]

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Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo. [Abstract]

2024 Apr 25;67(8):6658-6672. PMID: 38569135
Br J Cancer

Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer. [Abstract]

2022 Sep;127(5):927-936. PMID: 35618789
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Activators of the Anticipatory Unfolded Protein Response with Enhanced Selectivity for Estrogen Receptor Positive Breast Cancer. [Abstract]

2022 Mar 10;65(5):3894-3912. PMID: 35080871
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Protein Stability Effects in Aggregate-Based Enzyme Inhibition. [Abstract]

2019 Nov 14;62(21):9593-9599. PMID: 31589047
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Interaction of WBP2 with ERα increases doxorubicin resistance of breast cancer cells by modulating MDR1 transcription. [Abstract]

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Isoquercitrin Promotes Angiogenesis Through the Genomic Signaling Pathway of the Estrogen Receptor-Alpha. [Abstract]

2025 Oct;39(10):4802-4820. PMID: 40908639
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Environmental microcystin exposure triggers the poor prognosis of prostate cancer: Evidence from case-control, animal, and in vitro studies. [Abstract]

2023 May:127:69-81. PMID: 36522098
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Higher efficacy of resveratrol against advanced breast cancer organoids: A comparison with that of clinically relevant drugs. [Abstract]

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2023 Sep 15:263:115225. PMID: 37418940
Ecotoxicol Environ Saf

Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]

2021 Apr 1:212:111991. PMID: 33548570
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Organoids as a model system for researching human neuroendocrine tumor of the breast. [Abstract]

2024 Dec 27;24(1):433. PMID: 39731167
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2021 Feb;37(1):65-84. PMID: 32623698
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Mutant NPM1-regulated estrogen signaling promotes leukemia cell survival by upregulating HGF and represents a therapeutic vulnerability. [Abstract]

2026 May:247:117796. PMID: 41679667
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2025 Jul 16:241:117178. PMID: 40680865
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GNA13 suppresses proliferation of ER+ breast cancer cells via ERα dependent upregulation of the MYC oncogene. [Abstract]

2024 Jul 4;26(1):113. PMID: 38965558
Breast Cancer Res

Lasofoxifene as a potential treatment for aromatase inhibitor-resistant ER-positive breast cancer. [Abstract]

2024 Jun 7;26(1):95. PMID: 38849889
Biochem Pharmacol

MICAL-L2, as an estrogen-responsive gene, is involved in ER-positive breast cancer cell progression and tamoxifen sensitivity via the AKT/mTOR pathway. [Abstract]

2024 May 9:225:116256. PMID: 38729448
Breast Cancer Res

UCHL1 contributes to insensitivity to endocrine therapy in triple-negative breast cancer by deubiquitinating and stabilizing KLF5. [Abstract]

2024 Mar 11;26(1):44. PMID: 38468288
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Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. [Abstract]

2021 May 12;23(1):54. PMID: 33980285
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FGFR1 amplification or overexpression and hormonal resistance in luminal breast cancer: rationale for a triple blockade of ER, CDK4/6, and FGFR1. [Abstract]

2021 Feb 12;23(1):21. PMID: 33579347
Mol Cancer Ther

PKMYT1 is a Marker of Treatment Response and a Therapeutic Target for CDK4/6 Inhibitor-Resistance in ER+ Breast Cancer. [Abstract]

2024 May 23. PMID: 38781103
Inflammation

Large Peritoneal Macrophages Promote the Resolution of Inflammation in Injured Endometrium. [Abstract]

2025 Aug 2. PMID: 40751779
Int J Mol Sci

Estrogen-Mediated Regulation of Fam3d in Mouse Uterus During the Estrous Cycle. [Abstract]

2025 Dec 8;26(24):11840. PMID: 41465269
Int J Mol Sci

Bioinformatic-Experimental Screening Uncovers Multiple Targets for Increase of MHC-I Expression through Activating the Interferon Response in Breast Cancer. [Abstract]

2024 Sep 30;25(19):10546. PMID: 39408874
Biomolecules

Active Estrogen-Succinate Metabolism Promotes Heme Accumulation and Increases the Proliferative and Invasive Potential of Endometrial Cancer Cells. [Abstract]

2023 Jul 10;13(7):1097. PMID: 37509133
Eur J Pharmacol

Paeonol ameliorates postmenopausal hyperlipidemia by inhibiting COX-2 to suppress GRP78-mediated endoplasmic reticulum stress. [Abstract]

2026 Mar 28:1019:178736. PMID: 41796840
Eur J Pharmacol

Andrographolide analogues are agonists of the estrogen receptor alpha in vitro and in vivo. [Abstract]

2026 Feb 28:1016:178641. PMID: 41643829
Int Immunopharmacol

Estrogen deficiency promotes neurodegeneration in female hemi-parkinsonian mice: The role of regulatory T cells. [Abstract]

2025 Jan 24:148:114104. PMID: 39862633
Eur J Pharmacol

Syringaresinol attenuates sepsis-induced cardiac dysfunction by inhibiting inflammation and pyroptosis in mice. [Abstract]

2021 Dec 15:913:174644. PMID: 34801532
Reprod Biol Endocrinol

Upregulated Talin1 synergistically boosts β-estradiol-induced proliferation and pro-angiogenesis of eutopic and ectopic endometrial stromal cells in adenomyosis. [Abstract]

2021 May 14;19(1):70. PMID: 33990206
Mol Cancer Res

UBE2C Is Upregulated by Estrogen and Promotes Epithelial-Mesenchymal Transition via p53 in Endometrial Cancer. [Abstract]

2020 Feb;18(2):204-215. PMID: 31662448
Biosci Rep

Applying vibration in early postmenopausal osteoporosis promotes osteogenic differentiation of bone marrow-derived mesenchymal stem cells and suppresses postmenopausal osteoporosis progression. [Abstract]

2019 Sep 3;39(9):BSR20191011. PMID: 31406012
Am J Physiol Cell Physiol

cGMP-dependent protein kinase II determines β-catenin accumulation that is essential for uterine decidualization in mice. [Abstract]

2019 Dec 1;317(6):C1115-C1127. PMID: 31509448
Toxicology

Emerging organophosphate ester resorcinol bis(diphenyl phosphate) exerts estrogenic effects via estrogen receptor pathways. [Abstract]

2023 Nov:499:153649. PMID: 37827210
J Med Virol

Hepatitis E viral infection regulates estrogen signaling pathways: Inhibition of the cAMPK-PKA-CREB and PI3K-AKT-mTOR signaling pathways. [Abstract]

2021 Jun;93(6):3769-3778. PMID: 33128390
Toxicology

Estrogen receptor-regulated SOCS3 modulation via JAK2/STAT3 pathway is involved in BPF-induced M1 polarization of macrophages. [Abstract]

2020 Mar 30;433-434:152404. PMID: 32044397
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Aquat Toxicol

Inhibitory effects of estrogenic endocrine disrupting chemicals on fin regeneration in zebrafish are dependent on estrogen receptors. [Abstract]

2022 Jun;247:106156. PMID: 35405443
Exp Neurol

Biochanin A exerts neuroprotective effects in Parkinson's disease both in vivo and in vitro by improving mitochondrial dysfunction through the Sirt1 signaling pathway. [Abstract]

2026 Apr:398:115636. PMID: 41483847
Poult Sci

17β-estradiol mediates sex-biased progesterone receptor expression via estrogen receptor α in chicken pituitary. [Abstract]

2025 Dec 5;105(1):106210. PMID: 41380332
Mol Nutr Food Res

Diosmetin Protects Against Obesity and Metabolic Dysfunctions Through Activation of Adipose Estrogen Receptors in Mice. [Abstract]

2021 Sep;65(17):e2100070. PMID: 34223710
J Mol Med (Berl)

Klotho recovery by genistein via promoter histone acetylation and DNA demethylation mitigates renal fibrosis in mice. [Abstract]

2019 Apr;97(4):541-552. PMID: 30806715

Fulvestrant purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2019 Apr;97(4):541-552. [Abstract]

HK-2 cells treated with genistein (15 μM) and/or TGFβ (5 ng/ml) for 24 h are assayed with anti-acetylated and anti-total histone 3 antibodies by Western blot. In a separate assay, cell lysates treated with TGFβ and genistein in the presence or absence of Fulvestrant (Fulvest, 1 μM) under the same condition were also assayed. The quantifications are presented underneath the blots based on three independent experiments.
iScience

Multiomic characterization and drug testing establish circulating tumor cells as an ex vivo tool for personalized medicine. [Abstract]

2022 Sep 6;25(10):105081. PMID: 36204272
J Cell Physiol

17β-Estradiol mediates TGFBR3/Smad2/3 signaling to attenuate the fibrosis of TGF-β1-induced bovine endometrial epithelial cells via GPER. [Abstract]

2024 Jan;239(1):166-179. PMID: 37991438
Sci Rep

Icaritin alleviates motor impairment and osteoporosis in Parkinson's disease mice via the ER-PI3K/Akt pathway. [Abstract]

2025 Jan 25;15(1):3190. PMID: 39863664
Sci Rep

Proteomic profiling reveals that ESR1 mutations enhance cyclin-dependent kinase signaling. [Abstract]

2024 Mar 22;14(1):6873. PMID: 38519482
J Biol Chem

The AF-2 cofactor binding region is key for the selective SUMOylation of estrogen receptor alpha by antiestrogens. [Abstract]

2023 Jan;299(1):102757. PMID: 36460099
Metab Brain Dis

Astragalin alleviates cognitive deficits and neuronal damage in SAMP8 mice through upregulating estrogen receptor expression. [Abstract]

2022 Dec;37(8):3033-3046. PMID: 35984596
Naunyn Schmiedebergs Arch Pharmacol

Individual and combined antagonism of aryl hydrocarbon receptor (AhR) and estrogen receptors (ERs) offers distinct level of protection against Bisphenol A (BPA)-induced pancreatic islet cell toxicity in mice. [Abstract]

2025 Apr;398(4):3939-3954. PMID: 39377923
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Bioorg Med Chem

A novel selective estrogen receptor degrader induces cell cycle arrest in breast cancer via ERα degradation and the autophagy-lysosome pathway. [Abstract]

2023 Mar 15:82:117235. PMID: 36905762
Breast Cancer Res Treat

G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. [Abstract]

2020 Apr;180(3):635-646. PMID: 32130619
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Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]

2020 Jan;179(1):67-77. PMID: 31562570
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Causal links between programmed cell death and hypertrophic scars: Integrative analysis of multi-omics Mendelian randomization and preliminary experimental validation. [Abstract]

2025 Aug 19;51(8):107667. PMID: 40865488
Discov Oncol

Mucinous breast cancer organoids: an in vitro research model. [Abstract]

2025 May 19;16(1):814. PMID: 40388071
Toxicol Lett

Bisphenol F promotes the secretion of pro-inflammatory cytokines in macrophages by enhanced glycolysis through PI3K-AKT signaling pathway. [Abstract]

2021 Oct 10;350:30-39. PMID: 34147605
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Estrogenic Activity of Structurally Distinct PFASs Through Estrogen Receptor Pathway. [Abstract]

2025 Dec 1. PMID: 41326018
Mol Biol Rep

Acacetin improves endothelial dysfunction and aortic fibrosis in insulin-resistant SHR rats by estrogen receptors. [Abstract]

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High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]

2021 Feb;13(2):283-298. PMID: 32852861
PLoS One

Response Gene to Complement 32 promotes cell proliferation and tamoxifen resistance in breast cancer via elevated FoxM1 expression. [Abstract]

2025 Jul 28;20(7):e0328698. PMID: 40720499
PLoS One

Characterizing serotonin expression throughout bovine mammary gland developmental stages and its relationship with 17β-estradiol at puberty. [Abstract]

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Expression and Hormonal Regulation of Entpd3 at Various Estrous Cycle Stages in the Mouse Uterus. [Abstract]

2025 Apr;32(4):1033-1041. PMID: 39567465
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OBHSA, a novel selective estrogen receptor degrader, overcomes tamoxifen resistance through cell cycle arrest and unfolded protein response-mediated apoptosis in breast cancer. [Abstract]

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miR-192-5p suppresses uterine receptivity formation through impeding epithelial transformation during embryo implantation. [Abstract]

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Expression of purinergic receptor P2Y, G-protein coupled 2, is regulated by estrogen during the estrous cycle in mouse uterus. [Abstract]

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Icariin inhibits RANKL-induced osteoclastogenesis in RAW264.7 cells via inhibition of reactive oxygen species production by reducing the expression of NOX1 and NOX4. [Abstract]

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Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (412.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.12 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (3.43 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Solutol HS 15 10% Cremophor EL 35% PEG400 40% Water

Solubility: 2.5 mg/mL (4.12 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[3]

MCF-7 or T47D cells are cultured in 10 cm dishes to ~75% confluence in EMEM growth medium. Twenty-four hours before treatment, the growth medium is replaced with phenol red-free RPMI-1640 growth medium. A stock solution of 10 mM RAD1901 is prepared in DMSO. Dilutions of RAD1901 are prepared in RPMI growth medium (doses ranging from 10 to 0.5 nM). Controls include 0.1% DMSO alone (vehicle), 100 nM Fulvestrant, and 1 µM ICI 47699. Plated cells are treated with RAD1901 or controls for 48 h, and then incubated for 15 min with ice-cold lysis buffer [1 mM EDTA, 0.5% Triton X-100, 5 mM NaF, 6 M urea, 1 mM sodium orthovanadate, 2.5 mM sodium pyrophosphate, and 1× HALT protease inhibitor cocktail]. Lysates are centrifuged at 2000g for 5 min, and the supernatant is diluted 1 : 1 in lysis buffer. Ninety-six-well plates are coated overnight with capture antibody (1 µg/mL), washed three times in the manufacturer’s wash buffer, blocked with blocking buffer for 2 h, and washed again. The prepared plates are incubated with 100 µL of the prepared cell lysate for 2 h, washed, incubated with biotinylated detection antibody for 2 h, and washed again. After a 20 min incubation with streptavidin-horseradish peroxidase, the plates are washed and incubated with substrate solution for 20 min. The reaction is stopped with stop solution, and the plates are analyzed on a microplate reader (OD₄₅₀)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]^[3]

Rats^[1]
In studies with OVX rats, surgical preparation is performed at least 2 weeks before treatment began. To measure the duration of action of a single large dose of Fulvestrant, OVX rats are treated with a daily s.c. dose of 0.5 μg of estradici benzoate beginning on the day of Fulvestrant administration and continued until vaginal smears showed evidence of cornification. At that point the experiment is terminated and uterine weight is recorded. The arachis oil formulation used in these single dose duration of action studies contained 50 mg Fulvestrant/mL.
Mice^[3]
Female athymic nude mice [Crl:NU(NCr)-Foxn1nu] are used for tumor xenograft studies. Fourteen days after tumor cell implantation (designated as day 1 of the study), mice are 9 weeks of age, with body weights ranging from 21.4 to 32.5 g, individual tumor volumes ranging from 75 to 144 mm³, and a group mean tumor volume (MTV) of 108 mm³. The mice are randomized into nine groups of 15 animals each and treated with vehicle, ICI 47699 (1 mg/animal every other day), Fulvestrant (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week. The tumor endpoint is defined as an MTV of 1500 mm³ in the control group. Animals are also monitored for partial regression (PR) and complete regression responses.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (623 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51(15):3867-73. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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 [Content Brief]

[5]. Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27(7):1700-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6481 mL	8.2404 mL	16.4807 mL	41.2018 mL
	5 mM	0.3296 mL	1.6481 mL	3.2961 mL	8.2404 mL
	10 mM	0.1648 mL	0.8240 mL	1.6481 mL	4.1202 mL
	15 mM	0.1099 mL	0.5494 mL	1.0987 mL	2.7468 mL
	20 mM	0.0824 mL	0.4120 mL	0.8240 mL	2.0601 mL
	25 mM	0.0659 mL	0.3296 mL	0.6592 mL	1.6481 mL
	30 mM	0.0549 mL	0.2747 mL	0.5494 mL	1.3734 mL
	40 mM	0.0412 mL	0.2060 mL	0.4120 mL	1.0300 mL
	50 mM	0.0330 mL	0.1648 mL	0.3296 mL	0.8240 mL
	60 mM	0.0275 mL	0.1373 mL	0.2747 mL	0.6867 mL
	80 mM	0.0206 mL	0.1030 mL	0.2060 mL	0.5150 mL
	100 mM	0.0165 mL	0.0824 mL	0.1648 mL	0.4120 mL

Keywords

Fulvestrant

139 Cited Publications

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Fulvestrant

Apoptosis Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Lipid Compound Library

NMPA-Approved Drug Library

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Drug-Induced Liver Injury (DILI) Compound Library

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Mitochondrial Toxicity Compound Library

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Anti-Ovarian Cancer Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Human Hormone Compound Library

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Publications Citing Use of MedChemExpress (MCE) Fulvestrant

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR

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Chemical Information

Publications (139)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fulvestrant Related Classifications

Cat. No.: HY-13636