Tamoxifen Citrate
别名: ICI 46474, Istubal 中文名称：枸橼酸他莫昔芬
Tamoxifen Citrate是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。
Tamoxifen Citrate Chemical Structure
CAS: 54965-24-1
产品质控
批次：
纯度：
99.99%
99.99
Tamoxifen Citrate相关产品
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MCF7 | Antiproliferative assay | 3 mg/kg | 48 hrs | Antiproliferative activity against MCF7 cells at 3 mg/kg/day after 48 hrs, IC50=5.09μM | 16979337 |
| 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 |
| ER-positive MCF7 | Antiestrogenic assay | 20 nM | 48 hrs | Antiestrogenic activity in human ER-positive MCF7 cells assessed as inhibition of 17beta estradiol-induced secreted alkaline phosphatase activity at 20 nM after 48 hrs by phospha-light reporter chemiluminescence assay | 21800859 |
| C41 DE3 | Function assay | 60 uM | 10 mins | Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as modified apo-P450 2B6 adduct formation at 60 uM after 10 mins by ESI-LC-MS analysis in presence of NADPH | 22942317 |
| C41 DE3 | Function assay | 100 uM | 30 mins | Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as tryptic peptide 188FHYQDQE194 with site of adduct formation localized to Gln193 at 100 uM after 30 mins by LC-MS/MS analysis in presence of NADPH | 22942317 |
| MCF7 | Cytotoxicity assay | 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 |
| HCT116 | Function assay | 0.5 mM | 24 hrs | Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis | 23786452 |
| HeLa | Cytotoxicity assay | 10 mM | 48 hrs | Cytotoxicity against human HeLa cells assessed as reduction in cell viability in presence of 10 mM NAC after 48 hrs by WST8 assay | 25163667 |
| 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 | 18 hrs | Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced ERE promoter activation at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by luciferase reporter gene assay | 27088648 |
| MCF7 | Function assay | 3 to 10 uM | 18 hrs | Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced pS2 mRNA expression at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by RT-PCR analysis | 27088648 |
| MCF7 | Function assay | 10 nM | 24 hrs | Inhibition of ERalpha in human MCF7 cells assessed as reduction in 10 nM estrogen-induced progesterone receptor expression at 1 uM incubated for 24 hrs by Western blot method | 28942113 |
| MCF7 | Function assay | 1 uM | 4 hrs | Inhibition of ERalpha in human MCF7 cells assessed as downregulation of 17beta-estradiol-mediated pS2 mRNA expression at 1 uM preincubated for 4 hrs followed by 17beta-estradiol addition measured after 16 hrs by quantitative RT-PCR analysis | 29045135 |
| U2O2 | Function assay | 1 uM | 4 hrs | Inhibition of recombinant human GFP-fused ERalpha LBD (301 to 553 residues) expressed in human U2O2 cells assessed as downregulation of 17beta-estradiol-induced transcription at 1 uM preincubated for 4 hrs followed by E2 addition measured after 20 hrs by | 29045135 |
| MCF7 | Cell cycle assay | 10 uM | 24 to 48 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry | 29054359 |
| Ishikawa cells | Antiproliferative assay | >40 uM | 48 hrs | Antiproliferative activity against human Ishikawa cells at >40 uM after 48 hrs by MTT assay | 29482944 |
| MCF7 | Function assay | 60 mg/kg | 48 days | Downregulation of progesterone receptor mRNA level in NOD SCID gamma mouse xenografted with human MCF7 cells at 60 mg/kg, po 5 days per week for 48 days post tumor implantation measured 7 hrs post last dose by RT-PCR method | 29562737 |
| 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 |
| Lucena 1 | Function assay | 12.5 uM | 1 hr | Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry | 30613324 |
| Lucena 1 | Function assay | 25 uM | 1 hr | Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry | 30613324 |
| MCF7 | Cytotoxicity assay | 0.1 to 100 uM | 24 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay | 31514060 |
| BT-20 | Function assay | 10 uM | Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration, IC30=5.7μM | 2769681 | |
| MCF-7 | Function assay | 1 uM | Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30=6.5μM | 2769681 | |
| MCF-7 | Cytostaticity assay | 1 uM | Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50=8μM | 9089332 | |
| MCF-7 | Cytotoxicity assay | 1 uM | Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity=9.8μM | 9089332 | |
| MCF-7 | Cytotoxicity assay | 1 uM | Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity=13μM | 9089332 | |
| 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 | |
| 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 | |
| Neuro2a | Function assay | 1 uM | Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymostenol levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymosterol levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in cholesterol levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| Neuro2a | Function assay | 1 uM | Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | |
| MCF7 | Function assay | 1 uM | Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in estradiol-induced PgR mRNA expression at 1 uM by SYBR Green dye based RT-PCR analysis | 29482944 | |
| MCF7 | Function assay | 1 uM | Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in E2-induced progesterone receptor mRNA expression at 1 uM by SYBR green dye based RT-PCR method | 30384047 | |
| human Ishikawa cells | Cytotoxic assay | 18 h | Cytotoxicity against human Ishikawa cells after 18 hrs by MTT assay, IC50=12.5 μM | 19932024 | |
| human MDA-MB-231 cells | Cytotoxic assay | 18 h | Cytotoxicity against human MDA-MB-231 cells after 18 hrs by MTT assay, IC50=12.3 μM | 19932024 | |
| human MCF7 cells | Cytotoxic assay | 18 h | Cytotoxicity against human MCF7 cells after 18 hrs by MTT assay, IC50=10.2 μM | 19932024 | |
| human DU145 cells | Cytotoxic assay | 18 h | Cytotoxicity against human DU145 cells after 18 hrs by MTT assay, IC50=15.25 μM | 19932024 | |
| Ishikawa cells | Antiestrogenic assay | 4 days | Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 4 days by ELISA, IC50=0.42μM | 9784163 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against MCF7 cells after 72 hrs by MTT assay, Activity=4.6μM | 17918820 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50=0.58μM | 18272256 | |
| Ishikawa | Antiestrogenic assay | 72 hrs | Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 72 hrs, IC50=0.17μM | 18835176 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50=4.12μM | 18835176 | |
| T47D | Growth inhibition assay | 72 hrs | Growth inhibition of human estrogen-dependent T47D cells after 72 hrs, IC50=1μM | 19131248 | |
| HEK293 | Function assay | 30 mins | Stimulation of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis | 19136975 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=10μM | 19423356 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human estrogen receptor deficient MDA-MB-231 cells after 48 hrs by MTT assay, IC50=20μM | 19423356 | |
| MCF7 | Anticancer assay | 18 hrs | Anticancer activity against estrogen-positive human MCF7 cells after 18 hrs by MTT assay, IC50=12μM | 19446930 | |
| MDA-MB-231 | Anticancer assay | 18 hrs | Anticancer activity against estrogen-positive human MDA-MB-231 cells after 18 hrs by MTT assay, IC50=24μM | 19446930 | |
| NCI-H460 | Anticancer assay | 24 hrs | Anticancer activity against human NCI-H460 cells after 24 hrs by SRB assay, GI50=4.48μM | 19733085 | |
| DU145 | Anticancer assay | 24 hrs | Anticancer activity against human DU145 cells after 24 hrs by SRB assay, GI50=6.07μM | 19733085 | |
| SKOV3 | Anticancer assay | 24 hrs | Anticancer activity against human SKOV3 cells after 24 hrs by SRB assay, GI50=6.4μM | 19733085 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=7.65μM | 19740667 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=9.86μM | 19740667 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM | 19943620 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM | 19943620 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.2μM | 19943620 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 1 pM E2 after 96 hrs by alamar blue assay, Activity=0.4μM | 19943620 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.7μM | 19943620 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 1 pM E2 after 96 hrs by alamar blue assay, Activity=9μM | 19943620 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50=23.4μM | 20545334 | |
| HT-29 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HT-29 cells after 24 hrs by CellTiter-BlueCell viability assay, IC50=38.6μM | 20545334 | |
| MDA-MB-231 | Cytostatic activity assay | 3 days | Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay | 20598555 | |
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50=8.9μM | 20605470 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=10μM | 20605470 | |
| HEK293 | Cytotoxicity assay | 24 hrs | Cytotoxicity against HEK293 cells after 24 hrs by MTT assay, IC50=10μM | 20605470 | |
| HeLa | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50=12.5μM | 20605470 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=2.29087μM | 21513275 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=2.95121μM | 21513275 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=5.62341μM | 21513275 | |
| NCI-ADR-RES | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=5.7544μM | 21513275 | |
| MCF12A | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=5.7544μM | 21513275 | |
| MCF12A | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=5.7544μM | 21513275 | |
| MCF12A | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=6.91831μM | 21513275 | |
| NCI-ADR-RES | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=9.54993μM | 21513275 | |
| LNCAP | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=10μM | 21513275 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=10.9648μM | 21513275 | |
| NCI-ADR-RES | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=11.4815μM | 21513275 | |
| DU145 | Antiproliferative assay | 48 hrs | Antiproliferative activity against androgen receptor-deficient human DU145 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=13.8038μM | 21513275 | |
| HEK293 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, IC50=10μM | 21871812 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=12.48μM | 21871812 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against estrogen receptor-deficient human MDA-MB-231 cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=18.9μM | 21871812 | |
| Ishikawa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Ishikawa cells expressing estrogen receptor after 48 hrs by MTT assay, IC50=22.5μM | 21871812 | |
| HEK293 | Function assay | 1.5 hrs | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting, Ki=1.041μM | 22537153 | |
| AH109 | Function assay | 24 hrs | Antagonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay, IC50=1.66μM | 22647217 | |
| AH109 | Function assay | 24 hrs | Antagonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay, IC50=2.54μM | 22647217 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 24 hrs by MTT assay, IC50=19.54μM | 22647217 | |
| DLD1 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay, IC50=4.78μM | 22749392 | |
| MCF7 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50=7.1μM | 22749392 | |
| NIH/3T3 | Cytotoxicity assay | 96 hrs | Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50=7.26μM | 22749392 | |
| 518A2 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50=7.62μM | 22749392 | |
| A2780 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50=7.77μM | 22749392 | |
| Lipo | Cytotoxicity assay | 96 hrs | Cytotoxicity against human Lipo cells after 96 hrs by SRB assay, IC50=8.64μM | 22749392 | |
| A253 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human A253 cells after 96 hrs by SRB assay, IC50=8.92μM | 22749392 | |
| A549 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50=9.66μM | 22749392 | |
| 850C | Cytotoxicity assay | 96 hrs | Cytotoxicity against human 850C cells after 96 hrs by SRB assay, IC50=11.09μM | 22749392 | |
| KIF5 | Toxicity assay | 24 hrs | Toxicity against human KIF5 cells incubated for 24 hrs by CellTiter Blue cell viability assay, IC50=23.75μM | 22775474 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50=8.6μM | 22901895 | |
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells after 72 hrs by WST1 assay in presence of 20% FBS, IC50=14.3μM | 22901895 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=11.44μM | 23022281 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=12.41μM | 23022281 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay, IC50=1.82μM | 23123017 | |
| DU145 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50=5.5μM | 23287057 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=5.5μM | 23287057 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=6.3μM | 23287057 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50=10μM | 23287057 | |
| NIH/3T3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50=11.4μM | 23287057 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=11.4μM | 23287057 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=12μM | 23287057 | |
| T47D | Antiproliferative assay | 48 hrs | Antiproliferative activity against human T47D cells after 48 hrs by MTT assay, IC50=13μM | 23287057 | |
| MCF7 | Function assay | 6 days | Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method, IC50=0.2μM | 23448346 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50=12μM | 23735829 | |
| MSTO-211H | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MSTO-211H cells after 72 hrs by trypan blue assay, GI50=23.3μM | 23735829 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue assay, GI50=32.6μM | 23735829 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells expressing ERalpha and ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=15.6μM | 23786452 | |
| Vero | Cytotoxicity assay | 72 hrs | Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=15.9μM | 23786452 | |
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=17μM | 23786452 | |
| DU145 | Cytotoxicity assay | 72 hrs | Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=28.9μM | 23786452 | |
| Jurkat | Cytotoxicity assay | 48 hrs | Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay, IC50=8.3μM | 23792352 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=12.35μM | 23830503 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=27.96μM | 23860592 | |
| MCF7 | Cytotoxicity assay | 5 days | Cytotoxicity against human MCF7 cells after 5 days, IC50=0.794μM | 23864928 | |
| T47D | Cytotoxicity assay | 5 days | Cytotoxicity against human T47D cells after 5 days, IC50=1.13μM | 23864928 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=15.2μM | 23880359 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=13.45μM | 23902804 | |
| ScN2a-cl3 | Function assay | 5 days | Inhibition of RML prion protein infected in mouse dividing ScN2a-cl3 cells expressing full length mouse PrP assessed as reduction of PrPsc level after 5 days by ELISA, EC50=4.39μM | 24183589 | |
| ScN2a-cl3 | Cytotoxicity assay | 5 days | Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay, LC50=4.89μM | 24183589 | |
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50=9μM | 24457094 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=10μM | 24457094 | |
| HEK293 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay, IC50=26μM | 24457094 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.89μM | 24721727 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=6μM | 24880230 | |
| PC3 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay, IC50=7μM | 24880230 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=14μM | 24880230 | |
| MCF7 | Antiproliferative assay | 2 days | Antiproliferative activity human ER-positive MCF7 cells after 2 days by MTT assay, IC50=4.67μM | 25222876 | |
| MIAPaCa2 | Antiproliferative assay | 2 days | Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay, IC50=33.12μM | 25222876 | |
| MDA-MB-231 | Antiproliferative assay | 2 days | Antiproliferative activity human ER-negative MDA-MB-231 cells after 2 days by MTT assay, IC50=38.97μM | 25222876 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.1μM | 25369367 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs, GI50=5.2μM | 25420175 | |
| MCF7 | Antiproliferative assay | 5 days | Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50=2.1μM | 25614118 | |
| MCF7 | Antiproliferative assay | 3 days | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated at 37 degC for 3 days by resazurin microplate assay, IC50=18.71μM | 25734623 | |
| MCF7 | Antiproliferative assay | 48 hrs | Anti-proliferative activity against human MCF7 cells incubated for 48 hrs by SRB assay, GI50=8μM | 26163220 | |
| DU145 | Antiproliferative assay | 48 hrs | Anti-proliferative activity against human DU145 cells incubated for 48 hrs by SRB assay, GI50=19.3μM | 26163220 | |
| HepG2 | Antiproliferative assay | 48 hrs | Anti-proliferative activity against human HepG2 cells incubated for 48 hrs by SRB assay, GI50=21.7μM | 26163220 | |
| A549 | Antiproliferative assay | 48 hrs | Anti-proliferative activity against human A549 cells incubated for 48 hrs by SRB assay, GI50=24.4μM | 26163220 | |
| GBM2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=3.5μM | 26355532 | |
| GBM3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=4.7μM | 26355532 | |
| GBM1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=7.5μM | 26355532 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=1.58μM | 26896706 | |
| T47D | Cytotoxicity assay | 48 hrs | Cytotoxicity against human T47D cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=1.99μM | 26896706 | |
| MOLT4 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=2.5μM | 26896706 | |
| MDA-MB-468 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=2.5μM | 26896706 | |
| HCT15 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=3.16μM | 26896706 | |
| MDA-MB-435 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=3.16μM | 26896706 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.4μM | 26896706 | |
| SNB75 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=5.01μM | 26896706 | |
| EKVX | Cytotoxicity assay | 48 hrs | Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=6.3μM | 26896706 | |
| UO31 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=6.3μM | 26896706 | |
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50=10μM | 26896706 | |
| MRC5 | Cytotoxicity assay | 4 to 7 days | Cytotoxicity against human MRC5 cells assessed as cell viability after 4 to 7 days by Alamar Blue staining based fluorometric analysis, IC50=10.9μM | 26922226 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM | 27110635 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay, Activity=0.1μM | 27110635 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.3μM | 27110635 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay, Activity=0.9μM | 27110635 | |
| MCF7 | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 1 pM E2 after 96 hrs by alamar blue assay, Activity=4.5μM | 27110635 | |
| T47D | Antiestrogenic assay | 96 hrs | Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 1 pM E2 after 96 hrs by alamar blue assay, Activity=7μM | 27110635 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50=6.5μM | 27128175 | |
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by trypan blue assay, GI50=12μM | 27128175 | |
| A2780 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50=30.3μM | 27128175 | |
| OVCAR5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human OVCAR5 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50=32μM | 27128175 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50=5.3μM | 27176944 | |
| Ishikawa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Ishikawa cells incubated for 48 hrs by MTT assay, IC50=6μM | 27176944 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, IC50=13.9μM | 27176944 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against ER-positive human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by AlamarBlue assay, IC50=4.1μM | 27407030 | |
| SH-SY5Y | Function assay | 1 hr | Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis, IC50=20μM | 27647375 | |
| FADU | Anticancer assay | 48 hrs | Anticancer activity against human FADU cells measured after 48 hrs by SRB assay, IC50=5.39μM | 27671497 | |
| DLD1 | Anticancer assay | 48 hrs | Anticancer activity against human DLD1 cells measured after 48 hrs by SRB assay, IC50=11.06μM | 27671497 | |
| A549 | Anticancer assay | 48 hrs | Anticancer activity against human A549 cells measured after 48 hrs by SRB assay, IC50=17.3μM | 27671497 | |
| DU145 | Anticancer assay | 48 hrs | Anticancer activity against human DU145 cells measured after 48 hrs by SRB assay, IC50=18.07μM | 27671497 | |
| MCF7 | Anticancer assay | 48 hrs | Anticancer activity against human ER-positive MCF7 cells measured after 48 hrs by SRB assay, IC50=18.18μM | 27671497 | |
| MCF7 | Cytotoxicity assay | 120 hrs | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=6.8μM | 28152429 | |
| T47D | Cytotoxicity assay | 120 hrs | Cytotoxicity against human T47D cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=10.6μM | 28152429 | |
| SKBR3 | Cytotoxicity assay | 120 hrs | Cytotoxicity against human SKBR3 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=12.5μM | 28152429 | |
| MDA-MB-231 | Cytotoxicity assay | 120 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 120 hrs by MTT assay, GI50=15.1μM | 28152429 | |
| MCF7 | Function assay | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay, IC50=1.605μM | 28296398 | |
| Ishikawa cells | Function assay | 72 hrs | Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay, IC50=0.28μM | 28426931 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=4.1μM | 28426931 | |
| MCF7 | Cytotoxicity assay | 5 days | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by SRB assay, IC50=4.4μM | 28426931 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against ER positive human MCF7 cells after 48 hrs by MTT assay, IC50=11.35μM | 28460819 | |
| Ishikawa cells | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50=16.47μM | 28460819 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay, IC50=21.57μM | 28505536 | |
| HeLa | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=8.85μM | 28838694 | |
| HeLa | Function assay | 24 hrs | Antagonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay, IC50=0.341μM | 28882502 | |
| HeLa | Function assay | 24 hrs | Antagonist activity at full length ERbeta (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay, IC50=1.53μM | 28882502 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by resazurin based fluorescence assay, IC50=7.94μM | 28927795 | |
| insect cells | Function assay | 2 hrs | Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells incubated for 2 hrs by polarization, IC50=2.67μM | 28942113 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=14.35μM | 28942113 | |
| Ishikawa cells | Cytotoxicity assay | 48 hrs | Cytotoxicity in human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=20.65μM | 28942113 | |
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells assessed as cell viability up to 100 uM after 24 hrs by MTT assay | 29045135 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=8.12μM | 29054359 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=9.96μM | 29054359 | |
| HEK293 | Antiproliferative assay | 48 hrs | Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay, IC50=20.93μM | 29054359 | |
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50=5.3μM | 29220789 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=19.5μM | 29482944 | |
| MCF7 | Function assay | 24 hrs | Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay, IC50=1.605μM | 29562737 | |
| insect cells | Function assay | 2 hrs | Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells after 2 hrs by fluorescence polarization assay, IC50=1.42μM | 29587221 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=15.46μM | 29587221 | |
| Ishikawa cells | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay, IC50=26.52μM | 29587221 | |
| MRC5 SV2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MRC5 SV2 cells after 72 hrs by resazurin dye-based fluorimetric analysis, IC50=10.2μM | 29604541 | |
| MCF7 | Cytotoxicity assay | 4 hrs | Cytotoxicity against human MCF7 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=8.61μM | 29605808 | |
| DLD1 | Cytotoxicity assay | 4 hrs | Cytotoxicity against human DLD1 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=16.3μM | 29605808 | |
| A549 | Cytotoxicity assay | 4 hrs | Cytotoxicity against human A549 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay, IC50=17.3μM | 29605808 | |
| HeLa | Function assay | 4.5 hrs | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50=0.73μM | 29624387 | |
| MRC5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 72 hrs by resazurin assay, IC50=10μM | 29672041 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50=24.7μM | 30322754 | |
| HEK293 | Cytotoxicity assay | 24 hrs | Cytotoxicity against HEK293 cells after 24 hrs by resazurin dye-based fluorescence analysis, CC50=39.4μM | 30322754 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=7.09μM | 30360952 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=47.1μM | 30360952 | |
| insect cells | Function assay | 2 hrs | Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells measured after 2 hrs by fluorescence polarization assay, IC50=1.56μM | 30384047 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=16.7μM | 30384047 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50=12μM | 30613327 | |
| MRC5 SV2 | Cytotoxicity assay | 3 days | Cytotoxicity against human MRC5 SV2 cells after 3 days by resazurin dye based fluorescence assay, IC50=11.23μM | 30638761 | |
| MRC5 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MRC5 cells after 24 hrs by resazurin dye based assay, IC50=11.09μM | 30692024 | |
| T47D | Antiproliferative assay | 24 hrs | Antiproliferative activity against human T47D cells after 24 hrs by MTT assay, IC50=34.42μM | 30731397 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=42.4μM | 30731397 | |
| MRC5 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by resazurin dye based fluorimetric assay, CC50=11.09μM | 30857749 | |
| MRC5 | Cytotoxicity assay | 24 hrs | Cytotoxicity in human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay, IC50=11.09μM | 30879839 | |
| HEK293 | Cytotoxicity assay | 20 hrs | Cytotoxicity against HEK293 cells measured after 20 hrs by resazurin dye based fluorescence assay, IC50=24μM | 30975502 | |
| A2058 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay, EC50=12.5μM | 31099568 | |
| MelJuSo | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MelJuSo cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay, EC50=14.6μM | 31099568 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 Cells after 48 hrs by neutral red dye-based assay, IC50=4μM | 31129455 | |
| J774A.1 | Cytotoxicity assay | 24 hrs | Cytotoxicity against mouse J774A.1 cells assessed as reduction in cell viability incubated for 24 hrs by neutral red uptake assay, CC50=11.06μM | 31376569 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=22.6μM | 31620225 | |
| RAW264.7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 24 hrs by neutral red dye based assay, CC50=11.1μM | 31703818 | |
| MCF-7 | Function assay | Inhibition of [3H]thymidine incorporation into MCF-7 cells, IC50=7.2μM | 1573630 | ||
| MCF-7 | Function assay | Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50=0.00011μM | 2769681 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 8201587 | ||
| MCF-7 | Function assay | Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50=0.481μM | 9154963 | ||
| NIH-3T3-G185 | Function assay | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=6.4μM | 11716514 | ||
| NIH-3T3-G185 | Function assay | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=12.1μM | 11716514 | ||
| NIH-3T3-G185 | Function assay | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50=31.4μM | 11716514 | ||
| MCF-7-2a | Antiestrogenic assay | Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%, IC50=0.5μM | 12431063 | ||
| MCF-7-2a | Function assay | Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50=0.5μM | 12672249 | ||
| SK-E2 | Function assay | TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50=15.4μM | 12739759 | ||
| SK-E2 | Function assay | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50=23.3μM | 12739759 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 12825935 | ||
| MCF-7 | Function assay | Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50=0.58μM | 12825935 | ||
| Caco-2 | Function assay | TP_TRANSPORTER: transepithelial transport of Rhodamine 123 (basal to apical) in Caco-2 cells, IC50=29μM | 15386482 | ||
| HeLa | Function assay | Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay, IC50=0.622μM | 15658851 | ||
| MCF-7 | Antiproliferative assay | Antiproliferative activity in MCF-7 human breast cancer cells, IC50=2.3μM | 15658875 | ||
| MDA-MB 231 | Antiproliferative assay | Antiproliferative activity in MDA-MB 231 human breast cancer cells, IC50=10.6μM | 15658875 | ||
| insect cells | Function assay | Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50=0.07μM | 18835176 | ||
| insect cells | Function assay | Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50=0.17μM | 18835176 | ||
| T47D | Antiestrogenic assay | Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay, IC50=0.1μM | 19131248 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay, IC50=10.9μM | 19836230 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay, IC50=11.1μM | 19836230 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by WST-1 assay, IC50=11.4μM | 19836230 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells by WST-1 assay, IC50=12.4μM | 19836230 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50=0.66μM | 20451380 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50=1μM | 20451380 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 20621492 | ||
| HeLa | Function assay | Antagonist activity at human wild type ERalpha expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay | 20659801 | ||
| HeLa | Function assay | Transactivation of human wild type ERalpha expressed in human HeLa cells co-expressing AP-1 by luciferase reporter gene assay | 20659801 | ||
| HeLa | Function assay | Antagonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay | 20659801 | ||
| HeLa | Function assay | Agonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing AP-1 assessed as transactivation activity by luciferase reporter gene assay | 20659801 | ||
| MCF7 | Anticancer assay | Anticancer activity against human MCF7 cells expressing estrogen receptor by MTT assay, IC50=11.8μM | 20951035 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity activity against human MCF7 cells by MTS assay, IC50=31μM | 21680064 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 22472045 | ||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells, GI50=9.5μM | 23403084 | ||
| M21 | Growth inhibition assay | Growth inhibition of human M21 cells, GI50=11μM | 23403084 | ||
| MCF7 | Growth inhibition assay | Growth inhibition of estrogen-dependent human MCF7 cells, GI50=11.2μM | 23403084 | ||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of estrogen-independent human MDA-MB-231 cells, GI50=18.8μM | 23403084 | ||
| HL60 | Function assay | Inhibition of Delta(8)-Delta(7) sterol isomerase/Delta(24)-sterol reductase-mediated cholesterol biosynthesis in human HL60 cells assessed as increase in zymostenol and zymosterol accumulation | 23433667 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, IC50=5.19μM | 23806014 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay, IC50=3.8μM | 26079090 | ||
| MDA-MB-435S | Cytotoxicity assay | Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay, IC50=5.5μM | 26079090 | ||
| Vero | Cytotoxicity assay | Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay, IC50=5.7μM | 26079090 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells assessed as cell viability by MTT assay, IC50=8.4μM | 26079090 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=0.05754μM | 26407012 | ||
| MCF | Function assay | Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50=0.12882μM | 26407012 | ||
| MCF7 | Function assay | Antagonist activity at ERalpha receptor in human MCF7 cells, IC50=10μM | 26407012 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=13.7μM | 27155469 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells, IC50=17.9μM | 27155469 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by resazurin microplate assay, IC50=6.99μM | 27228159 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by resazurin microplate assay, IC50=19.33μM | 27311894 | ||
| insect cells | Function assay | Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay, IC50=0.222μM | 27647375 | ||
| insect cells | Function assay | Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor beta expressed in insect cells by fluorescence polarization assay, IC50=0.188μM | 28426931 | ||
| MCF7 | Cytostatic activity assay | Cytostatic activity against human MCF7 cells, IC50=2.7μM | 29207335 | ||
| insect | Function assay | Binding affinity to untagged human recombinant full length ERalpha expressed in insect cells 0.1 to 10000 uM by Fluormone ES2 Green displacement based assay | 30091920 | ||
| MDA-MB-231 | Function assay | Binding affinity to rRNA-A site in human MDA-MB-231 cells assessed as inhibition of protein translation, IC50=18.08μM | 30530174 | ||
| SiHa | Cytotoxicity assay | Cytotoxicity against human SiHa cells, GI50=0.12μM | 31200236 | ||
| PANC1 | Cytotoxicity assay | Cytotoxicity against human PANC1 cells, GI50=0.15μM | 31200236 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells, GI50=0.24μM | 31200236 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50=10.87μM | 31546197 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells by MTT assay, IC50=10.87μM | 31546197 | ||
| HeLa | Antiproliferative assay | Antiproliferative activity against human HeLa cells by MTT assay, IC50=10.87μM | 31546197 | ||
| DU145 | Antiproliferative assay | Antiproliferative activity against human DU145 cells by MTT assay, IC50=10.87μM | 31546197 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50=11.2μM | 31546197 | ||
| SiHa | Growth inhibition assay | Growth inhibition of human SiHa cells, GI50=0.12μM | 31605865 | ||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of human MDA-MB-231 cells, GI50=0.12μM | 31605865 | ||
| PANC1 | Growth inhibition assay | Growth inhibition of human PANC1 cells, GI50=0.12μM | 31605865 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by fluorescence based viable cell counting method, IC50=25μM | 31610378 | ||
| M-HeLa | Antiproliferative assay | Antiproliferative activity against human M-HeLa cells by fluorescence based viable cell counting method, IC50=28μM | 31610378 | ||
| Chang | Cytotoxicity assay | Cytotoxicity against human Chang cells assessed as reduction in cell viability by fluorescence based viable cell counting method, IC50=42.1μM | 31610378 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tamoxifen Citrate是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。 | |
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Tamoxifen具有抗雌激素活性(ER)而表现出抗肿瘤活性。在不同ER来源（种属），蛋白浓度和测定条件下，Tamoxifen对ER的表观亲和力在30到0.01%之间。Tamoxifen与ER的结合进一步引起抑制雌激素相关基因表达的抑制，包括被肿瘤通过自分泌或者旁分泌机制分泌的生长因子和血管生长因子。Tamoxifen也直接诱导细胞程序性死亡。[1] Tamoxifen抑制MCF-7细胞 [3H]胸腺嘧啶插入和DNA聚合酶活性，同时引起细胞DNA含量减少和细胞数目减少。Tamoxifen对MCF-7细胞生长的抑制作用可以通过在培养基中加入雌二醇逆转。2 和6 μM Tamoxifen降低S期细胞比例，增加G1期细胞比例。10 μM的Tamoxifen导致细胞在48小时内死亡。[2]Tamoxifen治疗10天后，抑制MCF-7的生长，IC50值为~10 nM。Tamoxifen抑制MCF-7的纤维蛋白溶解酶原激活性，并抑制雌二醇激活的纤维蛋白溶解酶原激活性。Tamoxifen也会引起细胞内孕酮受体水平小幅增加。[3]Tamoxifen抑制前列腺癌细胞系PC3, PC3-M和 DU145，IC50从5.5到10 μM，这与蛋白激酶C的抑制和p21的诱导相关。[4] |
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| 激酶实验 | 竞争性结合试验 | |||
| 从150平方厘米的T型瓶中收集细胞，蛋白以约2 mg/mL的浓度溶于PBS。180,000 ×g离心，上层清夜与不同浓度的Tamoxifen 和 2.5 nM [3H]雌二醇在0-4℃孵育16小时。用葡聚糖活性炭[l0 μL 0.5%葡聚糖 C-5% Norite A 的TE缓冲液]测定游离的类固醇。800×g，30分钟离心后测定。化合物的相对结合活性是以抑制50%放射性标记的雌二醇的浓度计算的，化合物对雌二醇的结合活性默认为100%。 | ||||
| 细胞实验 | 细胞系 | 人乳腺癌细胞MCF-7 | ||
| 浓度 | ~1 μM | |||
| 孵育时间 | 10天 | |||
| 方法 | MCF-7细胞接种于T-25烧瓶(1.5×105细胞/烧瓶)并在MEM中生长2天，MEM中含10 mM HEPES缓冲液，庆大霉素(50 微克/毫升)，青霉素(100 单位/毫升)，链霉素(0.1 毫克/毫升)，牛胰岛素(6 纳克/毫升)，氢化可的松(3.75 纳克/毫升)，以及用葡聚糖被覆活性炭在55 ℃下处理45分钟除去内生激素的5% 牛血清。随后将培养基更换为上诉的MEM，除了其包含2%活性炭葡聚糖处理的小牛血清和不同浓度的Tamoxifen。培养结束时，测定细胞数目。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CD36 / p-ERK / ERK p-AMPK / AMPK / p-ACC / ACC / p-P70S6K / p-S6 / p-4EBP1 ER-α66 / ER-α36 / HER2 / EGFR p-AKT / AKT |
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30573731 | |
| Immunofluorescence | CD36 |
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30573731 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在肿瘤中，Tamoxifen处理快速增殖的，雌二醇激活的MCF-7异种移植通过显著降肿瘤细胞增殖引起剂量依赖性的肿瘤生长阻滞或停止。Tamoxifen处理导致肿瘤生长减慢（肿瘤倍增时间，12天），显著延长了肿瘤倍增时间Tpot) (6.6天)，降低标记指数(%LI) (至8%)至处理后23天，而未处理的小鼠倍增时间是5天，Tpot是2.3 天，%LI 为23%。[5] Tamoxifen根据种属，组织和基因的不同，不仅具有抗雄性激素活性，还具有雌激素活性。Tamoxifen对骨和血清脂类浓度和子宫内膜等刺激有保护作用。[1] |
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| 动物实验 | Animal Models | 人乳腺癌异种移植MCF-7 |
| Dosages | 2cm三苯氧胺胶囊 | |
| Administration | 皮下植入 | |
| 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 |
化学信息&溶解度
| 分子量 | 563.64 | 分子式 | C26H29NO.C6H8O7 |
| CAS号 | 54965-24-1 | SDF | Download Tamoxifen Citrate SDF |
| Smiles | CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (177.41 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 49 mg/mL (86.93 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
I am wondering if the Tamoxifen (product Cat # S1972) is a 4-hydroxy Tamoxifen form or just plain Tamoxifen Citrate?
回答：
The Tamoxifen (S1972) is a prodrug, just plain Tamoxifen citrate.
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