4-Hydroxytamoxifen (Afimoxifene)
别名: Afimoxifene 中文名称：4-羟基三苯氧胺
4-Hydroxytamoxifen (Afimoxifene) 是tamoxifen的活性代谢产物，是一种选择性的雌激素受体调节分子，在乳腺癌的治疗和化学疗法中应用广泛。4-HT可激活intein-Cas9突变体的靶向修饰效率。
4-Hydroxytamoxifen (Afimoxifene) Chemical Structure
CAS: 68392-35-8
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纯度：
99.89%
99.89
4-Hydroxytamoxifen (Afimoxifene)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 | 0.625 nM | 24 hrs | Antiproliferative activity against human MCF7 cells at 0.625 nM after 24 hrs by MTS assay | 18272256 |
| MCF7 | Antiproliferative assay | 0.625 to 10 nM | 24 hrs | Antiproliferative activity against human MCF7 cells at >0.625 to 10 nM after 24 hrs by MTS assay | 18272256 |
| MCF7:WS8 | Antiestrogenic assay | 1 uM | 7 days | Antiestrogenic activity in human ERalpha expressing MCF7:WS8 cells assessed as inhibition of estradiol-induced proliferation at 1 uM after 7 days | 20334368 |
| MCF7 | Function assay | 1 μM | 6 days | Drug uptake in human MCF7 cells at 10'-6 M after 6 days by HPLC-MS/MS analysis | 23864928 |
| MCF7 | Function assay | 10 uM | 6 hrs | Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method | 24332630 |
| MCF7:WS8 | Function assay | 1 μM | 48 hrs | Agonist activity at ER in human MCF7:WS8 cells assessed as pS2 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis | 24805199 |
| MCF7:WS8 | Function assay | 1 μM | 48 hrs | Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis | 24805199 |
| GH3 | Function assay | 1 μM | 48 hrs | Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-6 M after 48 hrs by RT-PCR analysis | 24805199 |
| GH3 | Function assay | 0.1 nM to 1 μM | 48 hrs | Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-10 to 10'-6 M after 48 hrs by RT-PCR analysis | 24805199 |
| MCF7 | Anticancer assay | 250 to 500 nM | 5 days | Anticancer against human ER-positive MCF7 cells assessed as inhibition of estradiol-induced cell proliferation at 250 to 500 nM after 5 days | 24946145 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYC mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of TFF1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of GREB1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYBL2 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CCND1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CDC6 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of E2F1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| MCF7 | Function assay | 5 uM | 24 hrs | Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MKI67 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis | 30078609 |
| BT-20 | Function assay | 10 μM | Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration, IC30 = 4.8 μM. | 2769681 | |
| HEK293 | Function assay | 1 hr | Antagonist activity at recombinant human ERalpha expressed in HEK293 cells assessed as inhibition of estradiol-induced YFP-fused SRC1 coactivator recruitment measured after 1 hr in presence of Coelenterazine H by BRET assay, IC50 = 0.07 μM. | 30078609 | |
| HEK293 | Function assay | 30 mins | Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 0.044 μM. | 19136975 | |
| GT1-7 | Function assay | 20 to 24 hrs | Antagonist activity at estrogen receptor in mouse GT1-7 cells harboring beta-galactosidase reporter gene assessed as reduction in 17beta-estradiol induced response measured after 20 to 24 hrs by luciferase reporter gene assay, IC50 = 0.0332 μM. | 28400239 | |
| MCF7 | Cytotoxicity assay | 5 days | Cytotoxicity against human MCF7 cells after 5 days, IC50 = 0.0291 μM. | 23864928 | |
| 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 = 0.01 μM. | 28426931 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50 = 0.0085 μM. | 18272256 | |
| Rosetta 2 DE3 | Function assay | 1 hr | Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay, IC50 = 0.004 μM. | 28296398 | |
| 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 = 0.003 μM. | 28296398 | |
| MCF7 | Function assay | 4 hrs | Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal dextran-treated FBS incubated for 4 hrs by SP1 and anti-ER rabbit monocolnal antibody based in-cell Western assay, Activity = 0.0001 μM. | 30086626 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.107 μM. | 18835176 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50 = 0.107 μM. | 23735829 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.11 μM. | 28426931 | |
| T47D | Cytotoxicity assay | 5 days | Cytotoxicity against human T47D cells after 5 days, IC50 = 0.21 μM. | 23864928 | |
| CV1 | Function assay | 45 hrs | Inverse agonist activity at GAL4-DNA binding domain-fused mouse ERRgamma ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.6 μM. | 28189393 | |
| CV1 | Function assay | 45 hrs | Inverse agonist activity at GAL4-DNA binding domain-fused human ERRbeta ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.65 μM. | 28189393 | |
| 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 = 1.41254 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 = 1.90546 μM. | 21513275 | |
| 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 = 1.96 μM. | 29624387 | |
| MDA-MB-231 | Cytotoxicity assay | 4 days | Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 2.5 μM. | 30078609 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.79 μM. | 26896706 | |
| 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 = 3.23594 μM. | 21513275 | |
| MCF7 | Cytotoxicity assay | 4 days | Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 3.3 μM. | 30078609 | |
| 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 = 3.31131 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 = 3.46737 μM. | 21513275 | |
| MDA-MB-231 | Cytotoxicity assay | 4 days | Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.5 μM. | 30078609 | |
| 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 = 3.89045 μM. | 21513275 | |
| MCF7 | Cytotoxicity assay | 4 days | Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.9 μM. | 30078609 | |
| MCF10A | Cytotoxicity assay | 4 days | Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 4 μM. | 30078609 | |
| MCF10A | Cytotoxicity assay | 4 days | Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 4 μM. | 30078609 | |
| 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 = 4.46684 μM. | 21513275 | |
| Calu-1 | Function assay | 30 mins | Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 4.8 μM. | 19136975 | |
| MDA-MB-231 | Anticancer assay | 48 hrs | Anticancer against human ER-positive MDA-MB-231 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 5.4 μM. | 24946145 | |
| 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 = 6.16595 μM. | 21513275 | |
| AU565 | Anticancer assay | 48 hrs | Anticancer against human ER-negative AU565 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.2 μM. | 24946145 | |
| MCF7L | Anticancer assay | 48 hrs | Anticancer against human ER-positive MCF7L cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.3 μM. | 24946145 | |
| SKOV3-MDR1-M6/6 | Anticancer assay | 48 hrs | Anticancer against human SKOV3-MDR1-M6/6 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.49 μM. | 24946145 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 7.2 μM. | 24189055 | |
| SKOV3 | Anticancer assay | 48 hrs | Anticancer against human SKOV3 cells overexpressing P-gp assessed as cell viability after 48 hrs by SRB assay, IC50 = 7.46 μM. | 24946145 | |
| 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 = 7.58578 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 = 7.76247 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 = 8.31764 μM. | 21513275 | |
| MCF7 | Antiproliferative assay | 5 days | Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50 = 8.9 μM. | 25614118 | |
| MCF7 | Anticancer assay | 48 hrs | Anticancer against human ER-positive MCF7 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 9.2 μM. | 24946145 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 10.4 μM. | 24189055 | |
| MDA-MB-453 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. | 28506582 | |
| 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 = 10.7152 μM. | 21513275 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 13.6 μM. | 25618595 | |
| Vero | Antiproliferative assay | 72 hrs | Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.1 μM. | 25993269 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.3 μM. | 25993269 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 15.6 μM. | 28506582 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.6 μM. | 25993269 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 20.1 μM. | 28506582 | |
| MDA-MB-231 | Cytotoxicity assay | 3 days | Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay | 20598555 | |
| insect cells | Function assay | Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.04 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 = 0.02 μM. | 18835176 | ||
| MCF7 | Function assay | Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50 = 0.0085 μM. | 12825935 | ||
| MCF-7-2a | Function assay | Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50 = 0.007 μM. | 12672249 | ||
| insect cells | Function assay | Inhibition of fluormone ES2 green binding to recombinant full length human ERalpha expressed in insect cells by fluorescence polarization assay, IC50 = 0.00629 μM. | 28735214 | ||
| MCF7 | Function assay | Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50 = 0.00117 μM. | 9154963 | ||
| MCF | Function assay | Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50 = 0.0007943 μM. | 26407012 | ||
| Ishikawa endometrial cells | Function assay | Agonist activity as alkaline phosphatase induction in Ishikawa endometrial cells compared to E2, EC50 = 0.0008 μM. | 15380208 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50 = 0.000537 μM. | 26407012 | ||
| MCF7 | Function assay | Effective concentration against MCF-7 breast tumor cells using MCF-7 assay, EC50 = 0.00012 μM. | 12825935 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50 = 0.0005 μM. | 22405286 | ||
| MCF7 | Function assay | Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50 = 0.00003 μM. | 2769681 | ||
| MCF7 cells | Proliferation assay | Inhibition of estrogen-stimulated MCF-7 cell proliferation, IC50=0.5 nM | 9548817 | ||
| Ishikawa endometrial cells | Function assay | Antagonist activity as inhibition of 1 nM 17-beta-estradiol stimulated alkaline phosphatase induction in Ishikawa endometrial cells, IC50 = 0.51 μM. | 15380208 | ||
| HEK293 | Function assay | Agonist activity at human estrogen related receptor gamma expressed in HEK293 cells by luciferase reporter gene assay, IC50 = 1.35 μM. | 25305688 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells assessed as incorporation of [methyl-3H]thymidine into cellular DNA in serum free medium in in absence of 6.2 ug/mL RNase 1, IC50 = 2.7 μM. | 22611478 | ||
| MCF7 | Function assay | Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30 = 4 μM. | 2769681 | ||
| yeast cells | Antiestrogenic assay | Antiestrogenic activity at estrogen receptor alpha expressed in yeast cells assessed as inhibition of 17-beta-estradiol-induced beta-galactosidase activity by two hybrid assay, IC50 = 4.4 μM. | 16441086 | ||
| MCF7 | Function assay | Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 4.89779 μM. | 26407012 | ||
| MCF-7 | Cytotoxicity assay | Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity = 6 μM. | 9089332 | ||
| MCF-7 | Cytotoxicity assay | Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50 = 8 μM. | 9089332 | ||
| MCF-7 | Cytotoxicity assay | Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity = 9.4 μM. | 9089332 | ||
| MCF7:WS8 | Function assay | Activation of human ER in human MCF7:WS8 cells expressing estrogen responsive element by luciferase reporter gene assay | 20334368 | ||
| MCF7 | Antiestrogenic assay | Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated prolactin gene expression | 20334368 | ||
| MCF7 | Antiestrogenic assay | Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated proliferation | 20334368 | ||
| T47D:C:4:2 | Function assay | Estrogenic activity at wild type ER alpha expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay | 20334368 | ||
| T47D:C:4:2 | Function assay | Estrogenic activity at wild type ER alpha D351G mutant expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay | 20334368 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | 4-Hydroxytamoxifen (Afimoxifene) 是tamoxifen的活性代谢产物，是一种选择性的雌激素受体调节分子，在乳腺癌的治疗和化学疗法中应用广泛。4-HT可激活intein-Cas9突变体的靶向修饰效率。 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 4-OHT是有效的ER激活剂，它对雌激素受体有更高的亲和力。4-OHT具有较强的剂量和时间依赖式效应，能改变分离出来的大鼠心肌细胞的收缩功能[1]。4-HT可激活intein-Cas9突变体的靶向修饰效率[3]。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | 成年大鼠和小鼠心肌细胞 | ||
| 浓度 | 0, 0.5, 1, 3, 5, and 10 礛 | |||
| 孵育时间 | 15-45 min | |||
| 方法 | 细胞置于含有4OHT的台式液中，孵育温度为36 ± 1°C，以0.2Hz的频率予以刺激，测量其肌节长度。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-ERK / ERK / p-MEK / MEK1 / MEK2 / p21 / Cyclin D1 |
|
26163823 | |
| Growth inhibition assay | Cell viability |
|
26014809 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 | 387.51 | 分子式 | C26H29NO2 |
| CAS号 | 68392-35-8 | SDF | Download 4-Hydroxytamoxifen (Afimoxifene) SDF |
| Smiles | CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 77 mg/mL ( (198.7 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
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:
4-Hydroxytamoxifen (Afimoxifene) has two configurations, E and Z, which one does selleck provide?
回答：
According to the literature, the configuration of 4-Hydroxytamoxifen (Afimoxifene) does not affect its biological activity. S7827 is a mixture of E configuration and Z configuration, of which Z configuration accounts for more than 70%.
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