Home Endocrinology & Hormones Estrogen/progestogen Receptor modulator - Autophagy activator - Apoptosis related activator - HSP (HSP90) activator Tamoxifen Citrate For research use only.

Tamoxifen Citrate

Synonyms: ICI 46474, Istubal

Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

Tamoxifen Citrate Chemical Structure

Tamoxifen Citrate Chemical Structure

CAS: 54965-24-1

Selleck's Tamoxifen Citrate has been cited by 18 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells Cytotoxic assay 18 h Cytotoxicity against human MCF7 cells after 18 hrs by MTT assay, IC50=10.2 μM 19932024
human MDA-MB-231 cells Cytotoxic assay 18 h Cytotoxicity against human MDA-MB-231 cells after 18 hrs by MTT assay, IC50=12.3 μM 19932024
human Ishikawa cells Cytotoxic assay 18 h Cytotoxicity against human Ishikawa cells after 18 hrs by MTT assay, IC50=12.5 μM 19932024
human DU145 cells Cytotoxic assay 18 h Cytotoxicity against human DU145 cells after 18 hrs by MTT assay, IC50=15.25 μM 19932024
MCF-7 Function assay Inhibition of [3H]thymidine incorporation into MCF-7 cells, IC50=7.2μM 1573630
MCF-7 Function assay Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50=0.00011μM 2769681
BT-20 Function assay 10 uM Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration, IC30=5.7μM 2769681
MCF-7 Function assay 1 uM Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30=6.5μM 2769681
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 8201587
MCF-7 Cytostaticity assay 1 uM Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50=8μM 9089332
MCF-7 Cytotoxicity assay 1 uM Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity=9.8μM 9089332
MCF-7 Cytotoxicity assay 1 uM Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity=13μM 9089332
MCF-7 Function assay Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50=0.481μM 9154963
Ishikawa cells Antiestrogenic assay 4 days Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 4 days by ELISA, IC50=0.42μM 9784163
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=6.4μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=12.1μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50=31.4μM 11716514
MCF-7-2a Antiestrogenic assay Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%, IC50=0.5μM 12431063
MCF-7-2a Function assay Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50=0.5μM 12672249
SK-E2 Function assay TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50=15.4μM 12739759
SK-E2 Function assay TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50=23.3μM 12739759
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 12825935
MCF-7 Function assay Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50=0.58μM 12825935
Caco-2 Function assay TP_TRANSPORTER: transepithelial transport of Rhodamine 123 (basal to apical) in Caco-2 cells, IC50=29μM 15386482
HeLa Function assay Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay, IC50=0.622μM 15658851
MCF-7 Antiproliferative assay Antiproliferative activity in MCF-7 human breast cancer cells, IC50=2.3μM 15658875
MDA-MB 231 Antiproliferative assay Antiproliferative activity in MDA-MB 231 human breast cancer cells, IC50=10.6μM 15658875
MCF7 Function assay >10 uM Agonist activity at ERalpha assessed as inhibition of E2-induced luciferase gene transactivation in MCF7 cells at >10 uM 16735120
MCF7 Antiproliferative assay 3 mg/kg 48 hrs Antiproliferative activity against MCF7 cells at 3 mg/kg/day after 48 hrs, IC50=5.09μM 16979337
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against MCF7 cells after 72 hrs by MTT assay, Activity=4.6μM 17918820
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50=0.58μM 18272256
insect cells Function assay Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50=0.07μM 18835176
insect cells Function assay Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50=0.17μM 18835176
Ishikawa Antiestrogenic assay 72 hrs Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 72 hrs, IC50=0.17μM 18835176
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50=4.12μM 18835176
T47D Antiestrogenic assay Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay, IC50=0.1μM 19131248
T47D Growth inhibition assay 72 hrs Growth inhibition of human estrogen-dependent T47D cells after 72 hrs, IC50=1μM 19131248
HEK293 Function assay 30 mins Stimulation of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis 19136975
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=10μM 19423356
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human estrogen receptor deficient MDA-MB-231 cells after 48 hrs by MTT assay, IC50=20μM 19423356
MCF7 Anticancer assay 18 hrs Anticancer activity against estrogen-positive human MCF7 cells after 18 hrs by MTT assay, IC50=12μM 19446930
MDA-MB-231 Anticancer assay 18 hrs Anticancer activity against estrogen-positive human MDA-MB-231 cells after 18 hrs by MTT assay, IC50=24μM 19446930
NCI-H460 Anticancer assay 24 hrs Anticancer activity against human NCI-H460 cells after 24 hrs by SRB assay, GI50=4.48μM 19733085
DU145 Anticancer assay 24 hrs Anticancer activity against human DU145 cells after 24 hrs by SRB assay, GI50=6.07μM 19733085
SKOV3 Anticancer assay 24 hrs Anticancer activity against human SKOV3 cells after 24 hrs by SRB assay, GI50=6.4μM 19733085
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=7.65μM 19740667
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=9.86μM 19740667
MCF7 Cytotoxicity assay Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay, IC50=10.9μM 19836230
MCF7 Cytotoxicity assay Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay, IC50=11.1μM 19836230
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by WST-1 assay, IC50=11.4μM 19836230
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells by WST-1 assay, IC50=12.4μM 19836230
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM 19943620
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM 19943620
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.2μM 19943620
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 1 pM E2 after 96 hrs by alamar blue assay, Activity=0.4μM 19943620
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.7μM 19943620
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 1 pM E2 after 96 hrs by alamar blue assay, Activity=9μM 19943620
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50=0.66μM 20451380
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50=1μM 20451380
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50=23.4μM 20545334
HT-29 Cytotoxicity assay 24 hrs Cytotoxicity against human HT-29 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50=38.6μM 20545334
MDA-MB-231 Cytostatic activity assay 3 days Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay 20598555
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50=8.9μM 20605470
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=10μM 20605470
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against HEK293 cells after 24 hrs by MTT assay, IC50=10μM 20605470
HeLa Cytotoxicity assay 24 hrs Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50=12.5μM 20605470
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 20621492
HeLa Function assay 1 uM 48 hrs Antagonist activity at human ERalpha expressed in human HeLa cells coexpressing ERE-E1b-Luc assessed as inhibition of estradiol-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay 20621492
MCF7 Cytotoxicity assay 6 uM 96 hrs Cytotoxicity against human MCF7 cells assessed as reduction of cell proliferation at 6 uM after 96 hrs by MTT assay 20621492
HeLa Function assay Antagonist activity at human wild type ERalpha expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay 20659801
HeLa Function assay Transactivation of human wild type ERalpha expressed in human HeLa cells co-expressing AP-1 by luciferase reporter gene assay 20659801
HeLa Function assay Antagonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay 20659801
HeLa Function assay Agonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing AP-1 assessed as transactivation activity by luciferase reporter gene assay 20659801
MCF7 Anticancer assay Anticancer activity against human MCF7 cells expressing estrogen receptor by MTT assay, IC50=11.8μM 20951035
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=2.29087μM 21513275
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=2.95121μM 21513275
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=5.62341μM 21513275
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=5.7544μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=5.7544μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=5.7544μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=6.91831μM 21513275
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=9.54993μM 21513275
LNCAP Antiproliferative assay 48 hrs Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=10μM 21513275
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=10.9648μM 21513275
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=11.4815μM 21513275
DU145 Antiproliferative assay 48 hrs Antiproliferative activity against androgen receptor-deficient human DU145 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=13.8038μM 21513275
MCF7 Cytotoxicity assay Cytotoxicity activity against human MCF7 cells by MTS assay, IC50=31μM 21680064
ER-positive MCF7 Antiestrogenic assay 20 nM 48 hrs Antiestrogenic activity in human ER-positive MCF7 cells assessed as inhibition of 17beta estradiol-induced secreted alkaline phosphatase activity at 20 nM after 48 hrs by phospha-light reporter chemiluminescence assay 21800859
HEK293 Antiproliferative assay 48 hrs Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, IC50=10μM 21871812
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=12.48μM 21871812
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MDA-MB-231 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=18.9μM 21871812
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=22.5μM 21871812
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 22472045
HEK293 Function assay 1.5 hrs Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting, Ki=1.041μM 22537153
AH109 Function assay 24 hrs Antagonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay, IC50=1.66μM 22647217
AH109 Function assay 24 hrs Antagonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay, IC50=2.54μM 22647217
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 24 hrs by MTT assay, IC50=19.54μM 22647217
DLD1 Cytotoxicity assay 96 hrs Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay, IC50=4.78μM 22749392
MCF7 Cytotoxicity assay 96 hrs Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50=7.1μM 22749392
NIH/3T3 Cytotoxicity assay 96 hrs Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50=7.26μM 22749392
518A2 Cytotoxicity assay 96 hrs Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50=7.62μM 22749392
A2780 Cytotoxicity assay 96 hrs Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50=7.77μM 22749392
Lipo Cytotoxicity assay 96 hrs Cytotoxicity against human Lipo cells after 96 hrs by SRB assay, IC50=8.64μM 22749392
A253 Cytotoxicity assay 96 hrs Cytotoxicity against human A253 cells after 96 hrs by SRB assay, IC50=8.92μM 22749392
A549 Cytotoxicity assay 96 hrs Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50=9.66μM 22749392
850C Cytotoxicity assay 96 hrs Cytotoxicity against human 850C cells after 96 hrs by SRB assay, IC50=11.09μM 22749392
KIF5 Toxicity assay 24 hrs Toxicity against human KIF5 cells incubated for 24 hrs by CellTiter Blue cell viability assay, IC50=23.75μM 22775474
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50=8.6μM 22901895
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50=14.3μM 22901895
C41 DE3 Function assay 60 uM 10 mins Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as modified apo-P450 2B6 adduct formation at 60 uM after 10 mins by ESI-LC-MS analysis in presence of NADPH 22942317
C41 DE3 Function assay 60 uM Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as modified apo-P450 2B6 adduct formation at 60 uM by ESI-LC-MS analysis in presence of NADPH and GSHEE 22942317
C41 DE3 Function assay 100 uM 30 mins Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as tryptic peptide 188FHYQDQE194 with site of adduct formation localized to Gln193 at 100 uM after 30 mins by LC-MS/MS analysis in presence of NADPH 22942317
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=11.44μM 23022281
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=12.41μM 23022281
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay, IC50=1.82μM 23123017
DU145 Antiproliferative assay 48 hrs Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50=5.5μM 23287057
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=5.5μM 23287057
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=6.3μM 23287057
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50=10μM 23287057
NIH/3T3 Antiproliferative assay 48 hrs Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50=11.4μM 23287057
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=11.4μM 23287057
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=12μM 23287057
T47D Antiproliferative assay 48 hrs Antiproliferative activity against human T47D cells after 48 hrs by MTT assay, IC50=13μM 23287057
MCF7 Cytotoxicity assay 5 uM 48 hrs Cytotoxicity against human MCF7 cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay 23287057
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells, GI50=9.5μM 23403084
M21 Growth inhibition assay Growth inhibition of human M21 cells, GI50=11μM 23403084
MCF7 Growth inhibition assay Growth inhibition of estrogen-dependent human MCF7 cells, GI50=11.2μM 23403084
MDA-MB-231 Growth inhibition assay Growth inhibition of estrogen-independent human MDA-MB-231 cells, GI50=18.8μM 23403084
HL60 Function assay Inhibition of Delta(8)-Delta(7) sterol isomerase/Delta(24)-sterol reductase-mediated cholesterol biosynthesis in human HL60 cells assessed as increase in zymostenol and zymosterol accumulation 23433667
MCF7 Function assay 6 days Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method, IC50=0.2μM 23448346
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50=12μM 23735829
MSTO-211H Antiproliferative assay 72 hrs Antiproliferative activity against human MSTO-211H cells after 72 hrs by trypan blue assay, GI50=23.3μM 23735829
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue assay, GI50=32.6μM 23735829
HCT116 Function assay 0.5 mM 24 hrs Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis 23786452
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells expressing ERalpha and ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=15.6μM 23786452
Vero Cytotoxicity assay 72 hrs Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=15.9μM 23786452
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=17μM 23786452
DU145 Cytotoxicity assay 72 hrs Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=28.9μM 23786452
Jurkat Cytotoxicity assay 48 hrs Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay, IC50=8.3μM 23792352
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by SRB assay, IC50=5.19μM 23806014
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=12.35μM 23830503
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=27.96μM 23860592
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells after 5 days, IC50=0.794μM 23864928
T47D Cytotoxicity assay 5 days Cytotoxicity against human T47D cells after 5 days, IC50=1.13μM 23864928
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=15.2μM 23880359
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=13.45μM 23902804
ScN2a-cl3 Function assay 5 days Inhibition of RML prion protein infected in mouse dividing ScN2a-cl3 cells expressing full length mouse PrP assessed as reduction of PrPsc level after 5 days by ELISA, EC50=4.39μM 24183589
ScN2a-cl3 Cytotoxicity assay 5 days Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay, LC50=4.89μM 24183589
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50=9μM 24457094
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=10μM 24457094
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay, IC50=26μM 24457094
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.89μM 24721727
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=6μM 24880230
PC3 Antiproliferative assay 24 hrs Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay, IC50=7μM 24880230
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=14μM 24880230
HeLa Cytotoxicity assay 10 mM 48 hrs Cytotoxicity against human HeLa cells assessed as reduction in cell viability in presence of 10 mM NAC after 48 hrs by WST8 assay 25163667
MCF7 Antiproliferative assay 2 days Antiproliferative activity human ER-positive MCF7 cells after 2 days by MTT assay, IC50=4.67μM 25222876
MIAPaCa2 Antiproliferative assay 2 days Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay, IC50=33.12μM 25222876
MDA-MB-231 Antiproliferative assay 2 days Antiproliferative activity human ER-negative MDA-MB-231 cells after 2 days by MTT assay, IC50=38.97μM 25222876
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.1μM 25369367
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs, GI50=5.2μM 25420175
MCF7 Antiproliferative assay 5 days Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50=2.1μM 25614118
MCF7 Antiproliferative assay 3 days Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated at 37 degC for 3 days by resazurin microplate assay, IC50=18.71μM 25734623
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay, IC50=3.8μM 26079090
MDA-MB-435S Cytotoxicity assay Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay, IC50=5.5μM 26079090
Vero Cytotoxicity assay Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay, IC50=5.7μM 26079090
A549 Cytotoxicity assay Cytotoxicity against human A549 cells assessed as cell viability by MTT assay, IC50=8.4μM 26079090
MCF7 Antiproliferative assay 48 hrs Anti-proliferative activity against human MCF7 cells incubated for 48 hrs by SRB assay, GI50=8μM 26163220
DU145 Antiproliferative assay 48 hrs Anti-proliferative activity against human DU145 cells incubated for 48 hrs by SRB assay, GI50=19.3μM 26163220
HepG2 Antiproliferative assay 48 hrs Anti-proliferative activity against human HepG2 cells incubated for 48 hrs by SRB assay, GI50=21.7μM 26163220
A549 Antiproliferative assay 48 hrs Anti-proliferative activity against human A549 cells incubated for 48 hrs by SRB assay, GI50=24.4μM 26163220
GBM2 Antiproliferative assay 72 hrs Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=3.5μM 26355532
GBM3 Antiproliferative assay 72 hrs Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=4.7μM 26355532
GBM1 Antiproliferative assay 72 hrs Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=7.5μM 26355532
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50=0.05754μM 26407012
MCF Function assay Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50=0.12882μM 26407012
MCF7 Function assay Antagonist activity at ERalpha receptor in human MCF7 cells, IC50=10μM 26407012
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymostenol levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymosterol levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in cholesterol levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
AsPC1 Antiproliferative assay 10 uM 48 hrs Antiproliferative activity against human AsPC1 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay 26803204
BxPC3 Antiproliferative assay 10 uM 48 hrs Antiproliferative activity against human BxPC3 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay 26803204
MIAPaCa2 Antiproliferative assay 10 uM 48 hrs Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay 26803204
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=1.58μM 26896706
T47D Cytotoxicity assay 48 hrs Cytotoxicity against human T47D cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=1.99μM 26896706
MOLT4 Cytotoxicity assay 48 hrs Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=2.5μM 26896706
MDA-MB-468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=2.5μM 26896706
HCT15 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=3.16μM 26896706
MDA-MB-435 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=3.16μM 26896706
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.4μM 26896706
SNB75 Cytotoxicity assay 48 hrs Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=5.01μM 26896706
EKVX Cytotoxicity assay 48 hrs Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=6.3μM 26896706
UO31 Cytotoxicity assay 48 hrs Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=6.3μM 26896706
SKOV3 Cytotoxicity assay 48 hrs Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=10μM 26896706
MRC5 Cytotoxicity assay 4 to 7 days Cytotoxicity against human MRC5 cells assessed as cell viability after 4 to 7 days by Alamar Blue staining based fluorometric analysis, IC50=10.9μM 26922226
MCF7 Function assay 3 to 10 uM 18 hrs Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced ERE promoter activation at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by luciferase reporter gene assay 27088648
MCF7 Function assay 3 to 10 uM 18 hrs Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced pS2 mRNA expression at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by RT-PCR analysis 27088648
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM 27110635
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM 27110635
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.3μM 27110635
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.9μM 27110635
MCF7 Antiestrogenic assay 96 hrs Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 1 pM E2 after 96 hrs by alamar blue assay, Activity=4.5μM 27110635
T47D Antiestrogenic assay 96 hrs Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 1 pM E2 after 96 hrs by alamar blue assay, Activity=7μM 27110635
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50=6.5μM 27128175
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50=12μM 27128175
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50=30.3μM 27128175
OVCAR5 Cytotoxicity assay 72 hrs Cytotoxicity against human OVCAR5 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50=32μM 27128175
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50=13.7μM 27155469
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells, IC50=17.9μM 27155469
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50=5.3μM 27176944
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells incubated for 48 hrs by MTT assay, IC50=6μM 27176944
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, IC50=13.9μM 27176944
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by resazurin microplate assay, IC50=6.99μM 27228159
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by resazurin microplate assay, IC50=19.33μM 27311894
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER-positive human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by AlamarBlue assay, IC50=4.1μM 27407030
insect cells Function assay Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay, IC50=0.222μM 27647375
SH-SY5Y Function assay 1 hr Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis, IC50=20μM 27647375
FADU Anticancer assay 48 hrs Anticancer activity against human FADU cells measured after 48 hrs by SRB assay, IC50=5.39μM 27671497
DLD1 Anticancer assay 48 hrs Anticancer activity against human DLD1 cells measured after 48 hrs by SRB assay, IC50=11.06μM 27671497
A549 Anticancer assay 48 hrs Anticancer activity against human A549 cells measured after 48 hrs by SRB assay, IC50=17.3μM 27671497
DU145 Anticancer assay 48 hrs Anticancer activity against human DU145 cells measured after 48 hrs by SRB assay, IC50=18.07μM 27671497
MCF7 Anticancer assay 48 hrs Anticancer activity against human ER-positive MCF7 cells measured after 48 hrs by SRB assay, IC50=18.18μM 27671497
MCF7 Cytotoxicity assay 120 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=6.8μM 28152429
T47D Cytotoxicity assay 120 hrs Cytotoxicity against human T47D cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=10.6μM 28152429
SKBR3 Cytotoxicity assay 120 hrs Cytotoxicity against human SKBR3 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=12.5μM 28152429
MDA-MB-231 Cytotoxicity assay 120 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=15.1μM 28152429
MCF7 Function assay 24 hrs Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay, IC50=1.605μM 28296398
insect cells Function assay Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor beta expressed in insect cells by fluorescence polarization assay, IC50=0.188μM 28426931
Ishikawa cells Function assay 72 hrs Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay, IC50=0.28μM 28426931
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=4.1μM 28426931
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by SRB assay, IC50=4.4μM 28426931
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against ER positive human MCF7 cells after 48 hrs by MTT assay, IC50=11.35μM 28460819
Ishikawa cells Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50=16.47μM 28460819
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay, IC50=21.57μM 28505536
HeLa Cytotoxicity assay 24 hrs Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=8.85μM 28838694
HeLa Function assay 24 hrs Antagonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay, IC50=0.341μM 28882502
HeLa Function assay 24 hrs Antagonist activity at full length ERbeta (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay, IC50=1.53μM 28882502
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by resazurin based fluorescence assay, IC50=7.94μM 28927795
insect cells Function assay 2 hrs Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells incubated for 2 hrs by polarization, IC50=2.67μM 28942113
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=14.35μM 28942113
Ishikawa cells Cytotoxicity assay 48 hrs Cytotoxicity in human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=20.65μM 28942113
MCF7 Function assay 10 nM 24 hrs Inhibition of ERalpha in human MCF7 cells assessed as reduction in 10 nM estrogen-induced progesterone receptor expression at 1 uM incubated for 24 hrs by Western blot method 28942113
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells assessed as cell viability up to 100 uM after 24 hrs by MTT assay 29045135
MCF7 Function assay 1 uM 4 hrs Inhibition of ERalpha in human MCF7 cells assessed as downregulation of 17beta-estradiol-mediated pS2 mRNA expression at 1 uM preincubated for 4 hrs followed by 17beta-estradiol addition measured after 16 hrs by quantitative RT-PCR analysis 29045135
U2O2 Function assay 1 uM 4 hrs Inhibition of recombinant human GFP-fused ERalpha LBD (301 to 553 residues) expressed in human U2O2 cells assessed as downregulation of 17beta-estradiol-induced transcription at 1 uM preincubated for 4 hrs followed by E2 addition measured after 20 hrs by 29045135
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=8.12μM 29054359
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=9.96μM 29054359
HEK293 Antiproliferative assay 48 hrs Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay, IC50=20.93μM 29054359
MCF7 Cell cycle assay 10 uM 24 to 48 hrs Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry 29054359
MCF7 Cytostatic activity assay Cytostatic activity against human MCF7 cells, IC50=2.7μM 29207335
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50=5.3μM 29220789
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=19.5μM 29482944
Ishikawa cells Antiproliferative assay >40 uM 48 hrs Antiproliferative activity against human Ishikawa cells at >40 uM after 48 hrs by MTT assay 29482944
MCF7 Function assay 1 uM Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in estradiol-induced PgR mRNA expression at 1 uM by SYBR Green dye based RT-PCR analysis 29482944
MCF7 Function assay 24 hrs Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay, IC50=1.605μM 29562737
MCF7 Function assay 60 mg/kg 48 days Downregulation of progesterone receptor mRNA level in NOD SCID gamma mouse xenografted with human MCF7 cells at 60 mg/kg, po 5 days per week for 48 days post tumor implantation measured 7 hrs post last dose by RT-PCR method 29562737
insect cells Function assay 2 hrs Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells after 2 hrs by fluorescence polarization assay, IC50=1.42μM 29587221
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=15.46μM 29587221
Ishikawa cells Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50=26.52μM 29587221
MRC5 SV2 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 SV2 cells after 72 hrs by resazurin dye-based fluorimetric analysis, IC50=10.2μM 29604541
MCF7 Cytotoxicity assay 4 hrs Cytotoxicity against human MCF7 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=8.61μM 29605808
DLD1 Cytotoxicity assay 4 hrs Cytotoxicity against human DLD1 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=16.3μM 29605808
A549 Cytotoxicity assay 4 hrs Cytotoxicity against human A549 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=17.3μM 29605808
HeLa Function assay 4.5 hrs Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50=0.73μM 29624387
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 72 hrs by resazurin assay, IC50=10μM 29672041
MCF7 Antitumor assay 60 mg/kg 4 weeks Antitumor activity against human MCF7 cells xenografted in nu/nu mouse model of tamoxifen-sensitive breast cancer xenograft implanted with 17beta-estradiol time release pellets assessed as reduction tumor volume at 60 mg/kg, po qd for 4 weeks 30086626
insect Function assay Binding affinity to untagged human recombinant full length ERalpha expressed in insect cells 0.1 to 10000 uM by Fluormone ES2 Green displacement based assay 30091920
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50=24.7μM 30322754
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against HEK293 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50=39.4μM 30322754
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=7.09μM 30360952
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=47.1μM 30360952
insect cells Function assay 2 hrs Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells measured after 2 hrs by fluorescence polarization assay, IC50=1.56μM 30384047
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=16.7μM 30384047
MCF7 Function assay 1 uM Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in E2-induced progesterone receptor mRNA expression at 1 uM by SYBR green dye based RT-PCR method 30384047
MDA-MB-231 Function assay Binding affinity to rRNA-A site in human MDA-MB-231 cells assessed as inhibition of protein translation, IC50=18.08μM 30530174
Lucena 1 Function assay 12.5 uM 1 hr Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry 30613324
Lucena 1 Function assay 25 uM 1 hr Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry 30613324
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50=12μM 30613327
MRC5 SV2 Cytotoxicity assay 3 days Cytotoxicity against human MRC5 SV2 cells after 3 days by resazurin dye based fluorescence assay, IC50=11.23μM 30638761
MRC5 Cytotoxicity assay 24 hrs Cytotoxicity against human MRC5 cells after 24 hrs by resazurin dye based assay, IC50=11.09μM 30692024
T47D Antiproliferative assay 24 hrs Antiproliferative activity against human T47D cells after 24 hrs by MTT assay, IC50=34.42μM 30731397
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=42.4μM 30731397
MRC5 Cytotoxicity assay 24 hrs Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by resazurin dye based fluorimetric assay, CC50=11.09μM 30857749
MRC5 Cytotoxicity assay 24 hrs Cytotoxicity in human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay, IC50=11.09μM 30879839
HEK293 Cytotoxicity assay 20 hrs Cytotoxicity against HEK293 cells measured after 20 hrs by resazurin dye based fluorescence assay, IC50=24μM 30975502
A2058 Antiproliferative assay 24 hrs Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay, EC50=12.5μM 31099568
MelJuSo Antiproliferative assay 24 hrs Antiproliferative activity against human MelJuSo cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay, EC50=14.6μM 31099568
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 Cells after 48 hrs by neutral red dye-based assay, IC50=4μM 31129455
SiHa Cytotoxicity assay Cytotoxicity against human SiHa cells, GI50=0.12μM 31200236
PANC1 Cytotoxicity assay Cytotoxicity against human PANC1 cells, GI50=0.15μM 31200236
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells, GI50=0.24μM 31200236
J774A.1 Cytotoxicity assay 24 hrs Cytotoxicity against mouse J774A.1 cells assessed as reduction in cell viability incubated for 24 hrs by neutral red uptake assay, CC50=11.06μM 31376569
MCF7 Cytotoxicity assay 0.1 to 100 uM 24 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay 31514060
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50=10.87μM 31546197
A549 Antiproliferative assay Antiproliferative activity against human A549 cells by MTT assay, IC50=10.87μM 31546197
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by MTT assay, IC50=10.87μM 31546197
DU145 Antiproliferative assay Antiproliferative activity against human DU145 cells by MTT assay, IC50=10.87μM 31546197
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50=11.2μM 31546197
SiHa Growth inhibition assay Growth inhibition of human SiHa cells, GI50=0.12μM 31605865
MDA-MB-231 Growth inhibition assay Growth inhibition of human MDA-MB-231 cells, GI50=0.12μM 31605865
PANC1 Growth inhibition assay Growth inhibition of human PANC1 cells, GI50=0.12μM 31605865
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by fluorescence based viable cell counting method, IC50=25μM 31610378
M-HeLa Antiproliferative assay Antiproliferative activity against human M-HeLa cells by fluorescence based viable cell counting method, IC50=28μM 31610378
Chang Cytotoxicity assay Cytotoxicity against human Chang cells assessed as reduction in cell viability by fluorescence based viable cell counting method, IC50=42.1μM 31610378
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=22.6μM 31620225
RAW264.7 Cytotoxicity assay 24 hrs Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 24 hrs by neutral red dye based assay, CC50=11.1μM 31703818
Click to View More Cell Line Experimental Data

Biological Activity

Description Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
Targets
ER [1]
(Cell-free assay)
In vitro
In vitro

Tamoxifen displays antitumor effect due to its antiestrogenic activity (ER). Values for the apparent affinity of Tamoxifen for the ER range between 30 and 0.01% of that obtained for estradiol, dependent on different ER source (species), protein concentration and condition used for assay. Binding of Tamoxifen to ER further leads to inhibition expression of estrogen-regulated genes, including growth factors and angiogenic factors secreted by the tumor that may stimulate growth by autocrine or paracrine mechanisms. Tamoxifen also directly induces programmed cell death. [1] Tamoxifen produces an inhibitory effect on MCF-7 cell [3H]thymidine incorporation and DNA polymerase activity as well as causing a reduction in DNA content of cultures and cell numbers. This inhibitory effect of Tamoxifen on MCF-7 cell growth can be readily reversed by addition of estradiol to the culture medium. 2 and 6 μM Tamoxifen reduces the proportion of cells in S phase and increases the number of cells in G1. At 10 μM, Tamoxifen causes cell death within 48 hr. [2] Tamoxifen inhibits MCF-7 growth with IC50 of ~10 nM after 10 days treatment. Tamoxifen inhibits plasminogen activator activity of MCF-7, and suppresses estradiol-stimulation of plasminogen activator activity. Tamoxifen also evokes minimal increases in cellular progesterone receptor levels. [3] Tamoxifen is able to inhibit the growth of prostate cancer cell PC3, PC3-M, and DU145 with IC50 ranged from 5.5-10 μM, which is related to its inhibition of protein kinase C and induction of p21(waf1/cip1). [4]
Kinase Assay Competitive binding assays
Cells are harvested from 150-sq cm T-flasks, and cytosol is prepared at a protein concentration of approximately 2 mg/mL in phosphate buffer. Aliquots of this 180,000 ×g supernatant are then incubated with various concentrations of Tamoxifen and 2.5 nM [3H]estradiol for 16 hr at 0-4 ℃. The free steroids are absorbed by dextran-charcoal [l0 μL of 0.5% Dextran C-5% Norite A in TE buffer] for 1 hr at 0 ℃, and aliquots are counted after centrifugation at 800 ×g, 30 min. The relative binding ability of each competitor is taken as the ratio of the concentration of radioinert estradiol/competitor required to inhibit one-half of the specific [3H]estradiol binding, with the affinity of estradiol set at 100%.
Cell Research Cell lines Human breast cancer cells MCF-7
Concentrations ~1 μM
Incubation Time 10 days
Method

MCF-7 cells are seeded into T-25 flasks (1.5×105 cells/flask) and grown for 2 days in the MEM supplemented with 10 mM HEPES buffer, gentamicin (50 μg/mL), penicillin (100 units/mL), streptomycin (0.1 mg/mL), bovine insulin (6 ng/mL), hydrocortisone (3.75 ng/mL), and 5% calf serum that has been treated with dextran-coated charcoal for 45 min at 55 ℃ to remove endogenous hormones. The medium is then changed to MEM supplemented as described above, except that it contains 2% charcoal dextran-treated calf serum and various concentrations of Tamoxifen. At the end of incubation, cell numbers are counted.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT ER-α66 / ER-α36 / HER2 / EGFR p-AMPK / AMPK / p-ACC / ACC / p-P70S6K / p-S6 / p-4EBP1 CD36 / p-ERK / ERK 30759864
Immunofluorescence CD36 30573731
In Vivo
In vivo

Tamoxifen administration to rapidly growing, estradiol-stimulated MCF-7 xenografts results in a dose-dependent retardation or cessation of tumor growth by significantly decreasing tumor cell proliferation in tumor. Tamoxifen treatment results in a slowing of tumor growth (tumor doubling time, 12 days), a significant increase in tumor potential doubling time (Tpot) (6.6 days), and a decrease in labeling index (%LI) (to 8%) by 23 days posttreatment, compared with untreated mice which shows a volume doubling time of 5 days, a Tpot of 2.3 days, and a %LI of 23%. [5] Tamoxifen has not only antiestrogenic but also estrogenic properties depending on the species, tissue, and gene. Tamoxifen displays favorable effects on bone and serum lipid concentrations and stimulation endometrium. [1]
Animal Research Animal Models Human breast carcinoma xenografts MCF-7
Dosages 2 cm Tamoxifen capsules
Administration Subcutaneous implantation
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06154590 Not yet recruiting Metastatic Breast Cancer|Tumor|Muscle Neoplasms|Chronic Pain DR. DIANE CHISESI NFS. MD. PHD.|IRB|Paradyne Networks A Foundation July 2024 --
NCT05156892 Recruiting Ovarian Cancer Anthony Joshua FRACP|Royal Prince Alfred Hospital Sydney Australia|Concord Hospital|Prince of Wales Hospital Sydney|St Vincent''s Hospital Sydney September 4 2022 Phase 1
NCT04200066 Withdrawn Glioblastoma|Brain Tumor University of Rochester June 1 2022 Phase 1
NCT05133674 Active not recruiting Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast Karolinska University Hospital April 4 2022 Phase 2

Chemical lnformation & Solubility

Molecular Weight 563.64 Formula

C26H29NO.C6H8O7
CAS No. 54965-24-1 SDF Download Tamoxifen Citrate SDF
Smiles CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (177.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I am wondering if the Tamoxifen (product Cat # S1972) is a 4-hydroxy Tamoxifen form or just plain Tamoxifen Citrate?

Answer:
The Tamoxifen (S1972) is a prodrug, just plain Tamoxifen citrate.

Estrogen/progestogen Receptor Signaling Pathway Map

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