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Tamoxifen

Name: Tamoxifen
Brand: Selleck Chemicals
SKU: S1238
Rating: 5 (53 reviews)

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

Catalog No.S1238 Purity: 99.96%

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

CAS: 10540-29-1

Selleck's Tamoxifen has been cited by 53 publications

Purity & Quality Control

Batch: Purity: 99.96%

99.96

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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

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-CreER^Tm mice
	Dosages	--
	Administration	s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%absolute ethyl alcohol 1 95%Corn oil	5.0mg/ml (13.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	0.75mg/ml (2.02mM)	Taking the 1 mL working solution as an example, add 100 μL of 7.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	10%absolute ethyl alcohol 1 40%PEG300 2 5%Tween80 3 45%ddH2O	7.5mg/ml (20.19mM)	Taking the 1 mL working solution as an example, add 100 μL of 75 mg/ml clarified absolute ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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:
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):