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

Name: Fulvestrant
Brand: MedChemExpress
SKU: HY-13636
Rating: 5.0 (133 reviews)

Cat. No.: HY-13636 Purity: 99.98%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 129453-61-8

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Based on 133 publication(s) in Google Scholar

Other Forms of Fulvestrant:

133 Publications Citing Use of MCE Fulvestrant

IHC

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: 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.

: 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.

: 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.

: 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.

: 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.

: 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.

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Biological Activity
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Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
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	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]
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]
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]
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: 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	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: 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]
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]
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: 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	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	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	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	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	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	0.0015 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	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	0.12 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	0.16 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	0.16 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	0.29 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	0.32 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	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	IC₅₀	0.35 nM Compound: Fulvestrant	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 33138369]
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	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]
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	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	0.6 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 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	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	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	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	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	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	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	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	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	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	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	< 0.1 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]
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: 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]
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]
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	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	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	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 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	2.21 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	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	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	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	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	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	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]
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]

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.

Clinical Trial

Molecular Weight

606.77

Formula

C₃₂H₄₇F₅O₃S

CAS No.

129453-61-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (278 KB) SDS (623 KB)

COA (244 KB) HNMR (299 KB) RP-HPLC (255 KB) MS (70 KB) Elemental Analysis Report (101 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Fulvestrant Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fulvestrant129453-61-8ICI 182780 ZD 9238 ZM 182780ICI182780ICI-182780ZD9238ZD 9238ZD-9238ZM182780ZM 182780ZM-182780Estrogen Receptor/ERRAutophagyApoptosisInhibitorinhibitorinhibit

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

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