Home Angiogenesis Antineoplastic and Immunosuppressive Antibiotics chemical - Estrogen/progestogen Receptor modulator - Autophagy activator - HSP (HSP90) activator - ATPase activator - Apoptosis related activator Tamoxifen For research use only.

Tamoxifen

Synonyms: ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen

Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.

Tamoxifen Chemical Structure

Tamoxifen Chemical Structure

CAS No. 10540-29-1

Purity & Quality Control

Tamoxifen Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-435 cells Function assay Inhibition of MDA-MB-435 breast cancer cell proliferation, IC50=0.05 μM 14971899
MDA-MB-231 cells Function assay Inhibition of estrogen receptor negative MDA-MB-231 breast cancer cell proliferation, IC50=0.08 μM 14971899
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against MCF7 cells after 72 hrs by MTT assay, Activity = 4.6 μM. 17918820
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 = 0.1 μM. 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 = 0.1 μM. 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 = 0.2 μM. 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 = 0.4 μM. 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 = 0.7 μM. 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 = 9 μM. 19943620
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50 = 24.7 μM. 30322754
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against HEK293 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50 = 39.4 μM. 30322754
MCF-7 Cytotoxicity assay Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity = 9.8 μM. 9089332
MCF-7 Cytotoxicity assay Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity = 13 μM. 9089332
MCF-7 Function assay Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50 = 0.00011 μM. 2769681
Ishikawa Function assay Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells, EC50 = 0.033 μM. 8201587
MCF-7 Function assay Effective concentration against MCF-7 breast tumor cells using MCF-7 assay., EC50 = 0.01 μM. 12825935
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 = 4.39 μM. 24183589
NCI-H460 Anticancer assay 24 hrs Anticancer activity against human NCI-H460 cells after 24 hrs by SRB assay, GI50 = 4.48 μM. 19733085
DU145 Anticancer assay 24 hrs Anticancer activity against human DU145 cells after 24 hrs by SRB assay, GI50 = 6.07 μM. 19733085
SKOV3 Anticancer assay 24 hrs Anticancer activity against human SKOV3 cells after 24 hrs by SRB assay, GI50 = 6.4 μM. 19733085
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 = 2.29087 μM. 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 = 2.95121 μM. 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 = 5.62341 μM. 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 = 5.7544 μM. 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 = 5.7544 μM. 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 = 5.7544 μM. 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 = 6.91831 μM. 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 = 9.54993 μM. 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 = 10 μM. 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 = 10.9648 μM. 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 = 11.4815 μM. 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 = 13.8038 μM. 21513275
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells, GI50 = 9.5 μM. 23403084
M21 Growth inhibition assay Growth inhibition of human M21 cells, GI50 = 11 μM. 23403084
MCF7 Growth inhibition assay Growth inhibition of estrogen-dependent human MCF7 cells, GI50 = 11.2 μM. 23403084
MDA-MB-231 Growth inhibition assay Growth inhibition of estrogen-independent human MDA-MB-231 cells, GI50 = 18.8 μM. 23403084
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50 = 12 μM. 23735829
MSTO-211H Antiproliferative assay 72 hrs Antiproliferative activity against human MSTO-211H cells after 72 hrs by trypan blue assay, GI50 = 23.3 μM. 23735829
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue assay, GI50 = 32.6 μM. 23735829
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs, GI50 = 5.2 μM. 25420175
MCF7 Antiproliferative assay 48 hrs Anti-proliferative activity against human MCF7 cells incubated for 48 hrs by SRB assay, GI50 = 8 μM. 26163220
DU145 Antiproliferative assay 48 hrs Anti-proliferative activity against human DU145 cells incubated for 48 hrs by SRB assay, GI50 = 19.3 μM. 26163220
HepG2 Antiproliferative assay 48 hrs Anti-proliferative activity against human HepG2 cells incubated for 48 hrs by SRB assay, GI50 = 21.7 μM. 26163220
A549 Antiproliferative assay 48 hrs Anti-proliferative activity against human A549 cells incubated for 48 hrs by SRB assay, GI50 = 24.4 μM. 26163220
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 1.58 μM. 26896706
T47D Cytotoxicity assay 48 hrs Cytotoxicity against human T47D cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 1.99 μM. 26896706
MOLT4 Cytotoxicity assay 48 hrs Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 2.5 μM. 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 = 2.5 μM. 26896706
HCT15 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 3.16 μM. 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 = 3.16 μM. 26896706
SNB75 Cytotoxicity assay 48 hrs Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 5.01 μM. 26896706
EKVX Cytotoxicity assay 48 hrs Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 6.3 μM. 26896706
UO31 Cytotoxicity assay 48 hrs Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 6.3 μM. 26896706
SKOV3 Cytotoxicity assay 48 hrs Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 10 μM. 26896706
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50 = 6.5 μM. 27128175
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50 = 12 μM. 27128175
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 30.3 μM. 27128175
OVCAR5 Cytotoxicity assay 72 hrs Cytotoxicity against human OVCAR5 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 32 μM. 27128175
MCF7 Cytotoxicity assay 120 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50 = 6.8 μM. 28152429
T47D Cytotoxicity assay 120 hrs Cytotoxicity against human T47D cells assessed as growth inhibition after 120 hrs by MTT assay, GI50 = 10.6 μM. 28152429
SKBR3 Cytotoxicity assay 120 hrs Cytotoxicity against human SKBR3 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50 = 12.5 μM. 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 = 15.1 μM. 28152429
BT-20 Function assay 10 nM Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration., IC30 = 5.7 μM. 2769681
MCF-7 Function assay 1 nM Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30 = 6.5 μM. 2769681
MCF-7 Function assay Inhibition of [3H]thymidine incorporation into MCF-7 cells, IC50 = 7.2 μM. 1573630
MCF-7 Cytotoxicity assay Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50 = 8 μM. 9089332
MCF-7 Function assay Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50 = 0.481 μM. 9154963
Ishikawa 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 = 0.42 μM. 9784163
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50 = 6.4 μM. 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50 = 12.1 μM. 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50 = 31.4 μM. 11716514
MCF-7-2a Antiestrogenic assay Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%, IC50 = 0.5 μM. 12431063
MCF-7-2a Function assay Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50 = 0.5 μM. 12672249
SK-E2 Function assay TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50 = 15.4 μM. 12739759
SK-E2 Function assay TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50 = 23.3 μM. 12739759
MCF-7 Function assay Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay., IC50 = 0.58 μM. 12825935
Caco-2 Function assay TP_TRANSPORTER: transepithelial transport of Rhodamine 123 (basal to apical) in Caco-2 cells, IC50 = 29 μM. 15386482
HeLa Function assay Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay, IC50 = 0.622 μM. 15658851
MCF-7 Antiproliferative assay Antiproliferative activity in MCF-7 human breast cancer cells, IC50 = 2.3 μM. 15658875
MDA-MB 231 Antiproliferative assay Antiproliferative activity in MDA-MB 231 human breast cancer cells, IC50 = 10.6 μM. 15658875
MCF7 Antiproliferative assay 3 mg/kg/day 48 hrs Antiproliferative activity against MCF7 cells at 3 mg/kg/day after 48 hrs, IC50 = 5.09 μM. 16979337
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50 = 0.58 μM. 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 = 0.07 μM. 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 = 0.17 μM. 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 = 0.17 μM. 18835176
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 4.12 μM. 18835176
T47D Antiestrogenic assay Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay, IC50 = 0.1 μM. 19131248
T47D Growth inhibition assay 72 hrs Growth inhibition of human estrogen-dependent T47D cells after 72 hrs, IC50 = 1 μM. 19131248
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50 = 10 μM. 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 = 20 μM. 19423356
MCF7 Anticancer assay 18 hrs Anticancer activity against estrogen-positive human MCF7 cells after 18 hrs by MTT assay, IC50 = 12 μM. 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 = 24 μM. 19446930
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 7.65 μM. 19740667
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 9.86 μM. 19740667
MCF7 Cytotoxicity assay Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay, IC50 = 10.9 μM. 19836230
MCF7 Cytotoxicity assay Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay, IC50 = 11.1 μM. 19836230
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by WST-1 assay, IC50 = 11.4 μM. 19836230
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells by WST-1 assay, IC50 = 12.4 μM. 19836230
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50 = 0.66 μM. 20451380
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 1 μM. 20451380
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50 = 23.4 μM. 20545334
HT-29 Cytotoxicity assay 24 hrs Cytotoxicity against human HT-29 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50 = 38.6 μM. 20545334
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 8.9 μM. 20605470
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against HEK293 cells after 24 hrs by MTT assay, IC50 = 10 μM. 20605470
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 10 μM. 20605470
HeLa Cytotoxicity assay 24 hrs Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50 = 12.5 μM. 20605470
MCF7 Anticancer assay Anticancer activity against human MCF7 cells expressing estrogen receptor by MTT assay, IC50 = 11.8 μM. 20951035
MCF7 Cytotoxicity assay Cytotoxicity activity against human MCF7 cells by MTS assay, IC50 = 31 μM. 21680064
HEK293 Antiproliferative assay 48 hrs Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, IC50 = 10 μM. 21871812
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50 = 12.48 μM. 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 = 18.9 μM. 21871812
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells expressing estrogen receptor after 48 hrs by MTT assay, IC50 = 22.5 μM. 21871812
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.027 μM. 22472045
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 = 1.66 μM. 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 = 2.54 μM. 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 = 19.54 μM. 22647217
DLD1 Cytotoxicity assay 96 hrs Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay, IC50 = 4.78 μM. 22749392
MCF7 Cytotoxicity assay 96 hrs Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 7.1 μM. 22749392
NIH/3T3 Cytotoxicity assay 96 hrs Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 7.26 μM. 22749392
518A2 Cytotoxicity assay 96 hrs Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 7.62 μM. 22749392
A2780 Cytotoxicity assay 96 hrs Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 7.77 μM. 22749392
Lipo Cytotoxicity assay 96 hrs Cytotoxicity against human Lipo cells after 96 hrs by SRB assay, IC50 = 8.64 μM. 22749392
A253 Cytotoxicity assay 96 hrs Cytotoxicity against human A253 cells after 96 hrs by SRB assay, IC50 = 8.92 μM. 22749392
A549 Cytotoxicity assay 96 hrs Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 9.66 μM. 22749392
850C Cytotoxicity assay 96 hrs Cytotoxicity against human 850C cells after 96 hrs by SRB assay, IC50 = 11.09 μM. 22749392
KIF5 Toxicity assay 24 hrs Toxicity against human KIF5 cells incubated for 24 hrs by CellTiter Blue cell viability assay, IC50 = 23.75 μM. 22775474
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50 = 8.6 μM. 22901895
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50 = 14.3 μM. 22901895
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 11.44 μM. 23022281
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 12.41 μM. 23022281
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay, IC50 = 1.82 μM. 23123017
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 5.5 μM. 23287057
DU145 Antiproliferative assay 48 hrs Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50 = 5.5 μM. 23287057
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 6.3 μM. 23287057
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 10 μM. 23287057
NIH/3T3 Antiproliferative assay 48 hrs Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50 = 11.4 μM. 23287057
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 11.4 μM. 23287057
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 12 μM. 23287057
T47D Antiproliferative assay 48 hrs Antiproliferative activity against human T47D cells after 48 hrs by MTT assay, IC50 = 13 μM. 23287057
MCF7 Growth inhibition 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 = 0.2 μM. 23448346
HEK293T Function assay 20 hrs Antagonist activity at Gal4 DBD-fused human ERalpha LBD expressed in HEK293T cells assessed as inhibition of estradiol-induced transcriptional activation after 20 hrs by luciferase reporter gene assay, IC50 = 0.039 μM. 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 = 15.6 μM. 23786452
Vero Cytotoxicity assay 72 hrs Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 15.9 μM. 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 = 17 μM. 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 = 28.9 μM. 23786452
Jurkat Cytotoxicity assay 48 hrs Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay, IC50 = 8.3 μM. 23792352
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by SRB assay, IC50 = 5.19 μM. 23806014
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 12.35 μM. 23830503
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 27.96 μM. 23860592
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells after 5 days, IC50 = 0.794 μM. 23864928
T47D Cytotoxicity assay 5 days Cytotoxicity against human T47D cells after 5 days, IC50 = 1.13 μM. 23864928
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 15.2 μM. 23880359
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 13.45 μM. 23902804
MCF7 Cytotoxicity assay 24 hrs Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 9 μM. 24457094
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 10 μM. 24457094
HEK293 Cytotoxicity assay 24 hrs Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay, IC50 = 26 μM. 24457094
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 1.89 μM. 24721727
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 6 μM. 24880230
PC3 Antiproliferative assay 24 hrs Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay, IC50 = 7 μM. 24880230
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 14 μM. 24880230
MCF7 Antiproliferative assay 2 days Antiproliferative activity human ER-positive MCF7 cells after 2 days by MTT assay, IC50 = 4.67 μM. 25222876
MIAPaCa2 Antiproliferative assay 2 days Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay, IC50 = 33.12 μM. 25222876
MDA-MB-231 Antiproliferative assay 2 days Antiproliferative activity human ER-negative MDA-MB-231 cells after 2 days by MTT assay, IC50 = 38.97 μM. 25222876
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 4.1 μM. 25369367
MCF7 Antiproliferative assay 5 days Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50 = 2.1 μM. 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 = 18.71 μM. 25734623
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay, IC50 = 3.8 μM. 26079090
MDA-MB-435S Cytotoxicity assay Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay, IC50 = 5.5 μM. 26079090
Vero Cytotoxicity assay Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay, IC50 = 5.7 μM. 26079090
A549 Cytotoxicity assay Cytotoxicity against human A549 cells assessed as cell viability by MTT assay, IC50 = 8.4 μM. 26079090
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 = 3.5 μM. 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 = 4.7 μM. 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 = 7.5 μM. 26355532
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50 = 0.05754 μM. 26407012
MCF Function assay Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50 = 0.12882 μM. 26407012
MCF7 Function assay Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 10 μM. 26407012
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 4.4 μM. 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 = 10.9 μM. 26922226
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50 = 13.7 μM. 27155469
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells, IC50 = 17.9 μM. 27155469
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50 = 5.3 μM. 27176944
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells incubated for 48 hrs by MTT assay, IC50 = 6 μM. 27176944
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, IC50 = 13.9 μM. 27176944
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by resazurin microplate assay, IC50 = 6.99 μM. 27228159
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by resazurin microplate assay, IC50 = 19.33 μM. 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 = 4.1 μM. 27407030
insect cells Function assay 4 hrs 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 = 0.222 μM. 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 = 20 μM. 27647375
FADU Anticancer assay 48 hrs Anticancer activity against human FADU cells measured after 48 hrs by SRB assay, IC50 = 5.39 μM. 27671497
DLD1 Anticancer assay 48 hrs Anticancer activity against human DLD1 cells measured after 48 hrs by SRB assay, IC50 = 11.06 μM. 27671497
A549 Anticancer assay 48 hrs Anticancer activity against human A549 cells measured after 48 hrs by SRB assay, IC50 = 17.3 μM. 27671497
DU145 Anticancer assay 48 hrs Anticancer activity against human DU145 cells measured after 48 hrs by SRB assay, IC50 = 18.07 μM. 27671497
MCF7 Anticancer assay 48 hrs Anticancer activity against human ER-positive MCF7 cells measured after 48 hrs by SRB assay, IC50 = 18.18 μM. 27671497
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 = 1.605 μM. 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 = 0.188 μM. 28426931
Ishikawa Function assay 72 hrs Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay, IC50 = 0.28 μM. 28426931
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 4.1 μM. 28426931
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by SRB assay, IC50 = 4.4 μM. 28426931
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against ER positive human MCF7 cells after 48 hrs by MTT assay, IC50 = 11.35 μM. 28460819
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50 = 16.47 μM. 28460819
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay, IC50 = 21.57 μM. 28505536
HeLa Cytotoxicity assay 24 hrs Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 8.85 μM. 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 = 0.341 μM. 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 = 1.53 μM. 28882502
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by resazurin based fluorescence assay, IC50 = 7.94 μM. 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 = 2.67 μM. 28942113
MCF7 Cytotoxicity assay Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50 = 14.35 μM. 28942113
Ishikawa Cytotoxicity assay Cytotoxicity in human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50 = 20.65 μM. 28942113
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 8.12 μM. 29054359
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 9.96 μM. 29054359
HEK293 Antiproliferative assay 48 hrs Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay, IC50 = 20.93 μM. 29054359
MCF7 Cytotoxicity assay Cytostatic activity against human MCF7 cells, IC50 = 2.7 μM. 29207335
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50 = 5.3 μM. 29220789
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 19.5 μM. 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 = 1.605 μM. 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 = 1.42 μM. 29587221
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 15.46 μM. 29587221
Ishikawa Antiproliferative assay 48 hrs Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50 = 26.52 μM. 29587221
MRC5 SV2 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 SV2 cells after 72 hrs by resazurin dye-based fluorimetric analysis, IC50 = 10.2 μM. 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 = 8.61 μM. 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 = 16.3 μM. 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 = 17.3 μM. 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 = 0.73 μM. 29624387
MRC5 Cytotoxicity assay 72 hrs Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 72 hrs by resazurin assay, IC50 = 10 μM. 29672041
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 7.09 μM. 30360952
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 47.1 μM. 30360952
HeLa Function assay 18 hrs Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting, Ki = 0.03119 μM. 20621492
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 = 1.041 μM. 22537153
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 = 4.89 μM. 24183589
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
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
MDA-MB-231 Cytotoxicity assay 3 days Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay 20598555
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 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
Escherichia coli 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
Escherichia coli 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
Escherichia coli 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
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
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
HeLa Cytotoxicity assay 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
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 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 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 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
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 Function assay 3 to 10 uM 24 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 24 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 Function assay 1 uM 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 Function assay 1 uM 16 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
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
U2O2 Function assay 1 uM 20 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 Cell cycle arrest 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 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
Ishikawa 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 60 mg/kg 5 days per week for 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
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 cells Function assay 0.1 to 10000 uM 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
Click to View More Cell Line Experimental Data

Biological Activity

Description Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Targets
estrogen receptor [1]
In vitro
In vitro

TAM treatment inhibits significantly MCF7 cell proliferation. Low doses of TAM are able to induce structural chromosomal aberrations (deletions, isochromosomes, translocations, and dicentric chromosomes) in both ER+ and ER- breast cancer cells. This genotoxic effect is higher in those cell lines with HER2 gene amplification[2]. Whereas TAM at lower concentrations (0.1-1 μM) induces a cell-cycle arrest, pharmacological concentrations (above 5 μM) of TAM have been found to induce apoptosis of breast cancer cells. 5 μM TAM rapidly induced sustained activation of ERK1/2 in ER-positive breast cancer cell lines (MCF-7 and T47D)[3]
Cell Research Cell lines MCF7 and T47D
Concentrations 10-6 mol/L
Incubation Time 24, 48, and 96 h
Method

48 h before the addition of E2 and TAM, cells were washed with 5 mL phosphate-buffered saline (PBS) and then switched to phenol red-free RPMI-1640 containing 10% charcoal-stripped FBS. E2 and TAM were dissolved in absolute ethanol and diluted in the media at 10-8 mol/L and 10-6 mol/L, respectively, and then added to the culture medium at 24, 48, and 96 h.
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 (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver[2]. Tm-inducible Cre-loxP systems are being used in broad areas of research and are providing important biologic insights in tissue development, maintenance, and function. Tamoxifen-induced nuclear localization of Cre recombinase is time- and dose-dependent. Higher doses of tamoxifen induce recombination weeks following administration and Lower doses of tamoxifen induce recombination up to one week following administration. Duration of tamoxifen-induced gene recombination is also dose-dependent. Administration of high Tm doses leads to extended CreER nuclear localization. Tm treatment induces side effects that may have physiologic consequences in Tm-inducible models[4].
Animal Research Animal Models Pdx1PB-CreERTm mice
Dosages --
Administration s.c.
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 Unknown status
Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast
Karolinska University Hospital
 April 4 2022 Phase 2

Chemical Information & Solubility

Molecular Weight 371.51 Formula

C26H29NO
CAS No. 10540-29-1 SDF --
Smiles CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
Storage (From the date of receipt) 2 years 4°C, in dark and seal

In vitro
Batch:

Ethanol : 74 mg/mL

DMSO : 10 mg/mL ( (26.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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Frequently Asked Questions

Question 1:
Could you tell me if you have a protocol for the use of tamoxifen (S1238) in vivo in mouse? Is there an administration way that is better than another?

Answer:
Tamoxifen (S1238) can be dissolved in 10% ethanol/10% Tween 80/ddH2O at 5 mg/ml clearly. But precipitation will form if the formulation was left at RT for an hour or longer. So we'd suggest that you use it quickly after formulation. Tamoxifen is often administrated via i.p injection.

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