|(Z)-4-(1-(4-(2-(二甲氨基)乙氧基)苯基)-2-苯基-丁1-烯-1-基)苯酚|CsnPharm

CAS No.: 68047-06-3

4-羟基他莫昔芬 Catalog No. CSN22105

Synonyms: 4-羟基他莫昔芬;(Z)-4-Hydroxytamoxifen;trans-4-Hydroxytamoxifen

4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Estrogen receptors (ERs) play a key role in breast cancer progression. It is reported that 75% of women diagnosed with breast cancer have estrogen and progesterone receptor-positive breast tumors^[3]. 4-Hydroxytamoxifen (Afimoxifene, 4-OH-tamoxifen) is the active metabolite of tamoxifen and a selective estrogen receptor modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. 1 µM of 4-OH-tamoxifen treatment for 1h inhibited LM05-E and MCF-7 cells proliferation, and this effect was related to the PI3K/AKT pathway^[4]. In the MCF-7:5C cells, addition of 4-OH-tamoxifen at an equimolar concentration at early time points almost completely reversed the apoptosis induced by ethoxytriphenylethylene (10^-6 M) after 1 and 2 days of treatment^[5]. In vivo, three daily doses of 4-OH-tamoxifen (6 mg/day) effectively attenuated methamphetamine-induced nigrostriatal dopamine depletions in both sexes of intact and gonadectomized C57BL/6 J mice^[6].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
african green monkey Vero cells	-	Proliferation assay	72 h	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
BT-20 cells	-	Proliferation assay	-	Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration	2769681
Calu-1 cells	-	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

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临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01821066	Healthy	Phase 1	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Collapse <<
NCT00873366	-	-	Terminated(Funding issues)	-	United States, Arizona ... more >> Mayo Clinic in Arizona Scottsdale, Arizona, United States United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT00873366	-	-	Terminated(Funding issues)	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5806 mL
- 12.9029 mL
- 25.8058 mL
- 5 mM
- 0.5161 mL
- 2.5806 mL
- 5.1612 mL
- 10 mM
- 0.2581 mL
- 1.2903 mL
- 2.5806 mL

技术信息

CAS号

68047-06-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H29NO2

运输

蓝冰

分子量

387.51

别名

4-羟基他莫昔芬;(Z)-4-Hydroxytamoxifen;trans-4-Hydroxytamoxifen;(Z)-Afimoxifene

溶解度

DMSO	27.0 mg/mL (69.7 mM)
Water	Insoluble

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

african green monkey Vero cells	-	Proliferation assay	72 h	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
BT-20 cells	-	Proliferation assay	-	Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration	2769681
Calu-1 cells	-	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
DU145 cells	-	Proliferation assay	48 h	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
DU145 cells	-	Proliferation assay	72 h	Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50=15.3 μM	25993269
HEK293 cell	-	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
HEK293 cells	-	Function assay	-	Agonist activity at human estrogen related receptor gamma expressed in HEK293 cells by luciferase reporter gene assay, GI50=1.35 μM	25305688
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
LNCAP cells	-	Proliferation assay	48 h	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
MCF12A cells	-	Proliferation assay	48 h	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
MCF12A cells	-	Proliferation assay	48 h	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 cells	-	Proliferation assay	-	Inhibition of estrogen-stimulated MCF-7 cell proliferation, IC50=0.5 nM	9548817
MCF7 cells	-	Function assay	-	Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50=8.5 nM	12825935
MCF7 cells	-	Proliferation assay	72 h	Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50=0.107 μM	18835176
MCF7 cells	-	Proliferation assay	24 h	Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50=8.5 nM	18272256
MCF7 cells	10 μM	Function assay	6 h	Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method	24332630
MCF7 cells	-	Function assay	48 h	Anticancer against human ER-positive MCF7 cells assessed as cell viability after 48 hrs by SRB assay, IC50=9.2 μM	24946145
MCF7 cells	250 to 500 nM	Function assay	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 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=13.6 μM	25618595
MCF7:WS8 cells	-	Function assay	-	Activation of human ER in human MCF7:WS8 cells expressing estrogen responsive element by luciferase reporter gene assay	20334368
MCF7:WS8 cells	-	Function assay	48 h	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
MCF-7-2a cells	-	Function assay	-	Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50=0.007 μM	12672249
MDA-MB-231 cells	-	Function assay	3 days	Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay	20598555
MDA-MB-231 cells	-	Proliferation assay	24 h	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=10.4 μM	24189055
MDA-MB-231 cells	-	Function assay	48 h	Anticancer against human ER-positive MDA-MB-231 cells assessed as cell viability after 48 hrs by SRB assay, IC50=5.4 μM	24946145
MDA-MB-231 cells	-	Function assay	48 h	Anticancer against human ER-negative MDA-MB-231 cells assessed as cell viability after 48 hrs by SRB assay, IC50=6.2 μM	24946145
PC3 cells	-	Proliferation assay	48 h	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
rat GH3 cells	-	Function assay	48 h	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
rat GH3 cells	-	Function assay	48 h	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
SKOV3 cells	-	Function assay	48 h	Anticancer against human SKOV3 cells overexpressing P-gp assessed as cell viability after 48 hrs by SRB assay, IC50=7.46 μM	24946145
T47D cells	-	Cytotoxicity assay	5 days	Cytotoxicity against human T47D cells after 5 days, IC50=0.21 μM	23864928
T47D:C:4:2 cells	-	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

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01821066	Healthy	Phase 1	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Collapse <<
NCT00873366	-	-	Terminated(Funding issues)	-	United States, Arizona ... more >> Mayo Clinic in Arizona Scottsdale, Arizona, United States United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT00873366	-	-	Terminated(Funding issues)	-	-
NCT00963209	Breast Cancer	Phase 3	Unknown	December 2013	Switzerland ... more >> Hôpitaux Universitaire de Genève Recruiting Genève, Switzerland, 1211 Contact: Alexandre Bodmer, MD 41 22 382 40 14 Centre Hospitalier Universitaire Vaudois Recruiting Lausanne, Switzerland, 1011 Contact: Khalil Zaman, MD 41-21-314-0168 Khalil.Zaman@chuv.ch Collapse <<
NCT01189500	-	-	Completed	-	-
NCT03423199	Breast Neoplasms	Phase 3	Recruiting	February 2022	Japan ... more >> Aichi Cancer Center Hospital Recruiting Nagoya, Aichi, Japan, 464-8681 Contact: Hiroji Iwata, MD National Cancer Center Hospital East Recruiting Kashiwa, Chiba, Japan, 2778577 Contact: Hirofumi Mukai, MD, PhD National Hospital Organization Shikoku Cancer Center Recruiting Matsuyama, Ehime, Japan, 7910280 Contact: Kenjiro Aogi National Hospital Organization Hokkaido Cancer Center Recruiting Sapporo, Hokkaido, Japan, 0030804 Contact: Masato Takahashi, MD, PhD Hyogo Cancer Center Recruiting Akashi, Hyogo, Japan, 6738558 Contact: Koji Matsumoto, MD Kanagawa Cancer Center Recruiting Yokohama, Kanagawa, Japan, 2418515 Contact: Toshinari Yamashita, MD, PhD Kindai University Hospital Recruiting Ōsaka-sayama, Osaka, Japan, 5898511 Contact: Junji Tsurutani, MD, PhD Toranomon Hospital Recruiting Minato-Ku, Tokyo, Japan, 1058470 Contact: Toshimi Takano, MD Chiba Cancer Center Recruiting Chiba, Japan, 2608717 Contact: Naohito Yamamoto, MD, PhD Kyusyu Cancer Center Recruiting Fukuoka, Japan, 8111395 Contact: Eriko Tokunaga, MD National Hospital Organization Osaka National Hospital Recruiting Osaka, Japan, 5400006 Contact: Norikazu Masuda National Cancer Center Hospital Recruiting Tokyo, Japan, 104-0045 Contact: Kenji Tamura, MD, PhD Korea, Republic of National Cancer Center Recruiting Gyeonggi-do, Korea, Republic of, 10408 Contact: Keun Seok Lee, MD, PhD Ajou University Hospital Recruiting Gyeonggi-do, Korea, Republic of, 16499 Contact: Seok Yun Kang, MD Seoul National University Bundang Hospital Recruiting Gyeonggi-do, Korea, Republic of, 463-707 Contact: Jee Hyun Kim, MD, MS, PhD Seoul National University Hospital Recruiting Seoul, Korea, Republic of, 03080 Contact: Kyung-Hun Lee, MS, PhD Asan Medical Center Recruiting Seoul, Korea, Republic of, 05505 Contact: Kyung Hae Jung, MD, PhD Severance Hospital, Yonsei University Health System Recruiting Soeul, Korea, Republic of, 03722 Contact: Joo Hyuk Sohn, MD Singapore National University Hospital Recruiting Singapore, Singapore, 119882 Contact: Soo Chin Lee, MMed, MRCP National Cancer Centre Singapore Recruiting Singapore, Singapore, 169610 Contact: Yoon Sim Yap, MD Taiwan National Taiwan University Hospital Recruiting Taipei, Taiwan, 10048 Contact: Yen-Shen Lu, PhD Taipei Vetarans General Hospital Recruiting Taipei, Taiwan, 11217 Contact: Ling-Ming Tseng, MD Sun Yat-Sen Cancer Center Recruiting Taipei, Taiwan, 11259 Contact: Mei-Ching Liu, MD Collapse <<
NCT01864642	Ocular Hypertension ... more >> Glaucoma Collapse <<	Not Applicable	Completed	-	United States, Wisconsin ... more >> UW Dept of Ophthalmology Clinic Madison, Wisconsin, United States, 53715 Collapse <<
NCT00667121	-	-	Active, not recruiting	November 2018	United States, Indiana ... more >> Indiana University Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202-5289 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231-2410 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109-0942 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT00084344	Breast Cancer	Not Applicable	Completed	-	United States, Illinois ... more >> Robert H. Lurie Comprehensive Cancer Center at Northwestern University Chicago, Illinois, United States, 60611 Collapse <<
NCT01189500	Pharmacokinetics	Phase 4	Completed	-	United States, Florida ... more >> Pfizer Investigational Site Miami, Florida, United States, 33126 Pfizer Investigational Site Miami, Florida, United States, 33134 Collapse <<
NCT00272714	Cyclic Breast Pain, Cyclic Mas... more >>talgia Collapse <<	Phase 2	Completed	-	-
NCT03582865	-	-	Not yet recruiting	December 2019	-
NCT00952731	Ductal Breast Carcinoma in Sit... more >>u Estrogen Receptor-positive Breast Cancer Collapse <<	Phase 2	Completed	-	United States, Illinois ... more >> Northwestern University Chicago, Illinois, United States, 60611 Collapse <<
NCT00952731	-	-	Completed	-	-
NCT02993159	Ductal Breast Carcinoma In Sit... more >>u Estrogen Receptor Positive Collapse <<	Phase 2	Recruiting	July 15, 2019	United States, Illinois ... more >> Northwestern University Recruiting Chicago, Illinois, United States, 60611 Contact: Seema A. Khan, MD 312-503-4236 skhan@nm.org Principal Investigator: Seema A. Khan, MD United States, Kentucky Saint Elizabeth Medical Center South Recruiting Edgewood, Kentucky, United States, 41017 Contact: Joseph M. Guenther, MD 859-344-1600 Joseph.Guenther@stelizabeth.com Principal Investigator: Joseph M. Guenther, MD United States, Minnesota Mayo Clinic Not yet recruiting Rochester, Minnesota, United States, 55905 Contact: Amy C. Degnim, MD 507-284-4499 degnim.amy@mayo.edu Principal Investigator: Amy C. Degnim, MD United States, New York Memorial Sloan-Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Melissa L. Pilewskie, MD 646-888-4590 pilewskm@mskcc.org Principal Investigator: Melissa L. Pilewskie, MD United States, North Carolina Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Eun-Sil (Shelley) Hwang, MD 919-684-6849 shelly.hwang@duke.edu Principal Investigator: Eun-Sil (Shelley) Hwang, MD United States, Ohio Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44106 Contact: Stephen R. Grobmyer, MD 216-636-2843 grobmys@ccf.org Principal Investigator: Stephen R. Grobmyer, MD Collapse <<
NCT03063619	Mammographically Dense Breast	Phase 2	Recruiting	May 15, 2019	United States, Florida ... more >> Moffitt Cancer Center Not yet recruiting Tampa, Florida, United States, 33612 Contact: Nagi B. Kumar 813-745-6885 nagi.kumar@moffitt.org Principal Investigator: Nagi B. Kumar United States, Illinois Northwestern University Not yet recruiting Chicago, Illinois, United States, 60611 Contact: Seema A. Khan 312-503-4236 s-khan2@northwestern.edu Principal Investigator: Seema A. Khan United States, Massachusetts Dana-Farber Cancer Institute Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Judy E. Garber 617-632-5770 Judy_Garber@dfci.harvard.edu Principal Investigator: Judy E. Garber United States, New York Columbia University/Herbert Irving Cancer Center Not yet recruiting New York, New York, United States, 10032 Contact: Katherine D. Crew 212-305-1732 kd59@cumc.columbia.edu Principal Investigator: Katherine D. Crew United States, Texas M D Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Powel H. Brown 713-792-4509 phbrown@mdanderson.org Principal Investigator: Powel H. Brown Collapse <<
NCT03199963	Mammographic Breast Density	Phase 3	Recruiting	October 30, 2020	United States, Arizona ... more >> Mesa Obstetricians and Gynecologists/Cactus Clinical Research Recruiting Mesa, Arizona, United States, 85209 Contact: Study Coordinator Visions Clinical Research Recruiting Tucson, Arizona, United States, 85712 Contact: Study Coordinator United States, California United Clinical Research Recruiting Beverly Hills, California, United States, 90211 Contact: Study Coordinator City of Hope Recruiting Duarte, California, United States, 91010 Contact: Study Coordinator USC-Keck Medical Center Recruiting Los Angeles, California, United States, 90033 United States, Florida South Florida Medical Research Recruiting Aventura, Florida, United States, 33180 Contact: Study Coordinator Lake OB-GYN Associates of Mid-Florida Recruiting Leesburg, Florida, United States, 34748 Contact: Study Coordinator Physician Care Clinical Research, LLC Recruiting Sarasota, Florida, United States, 34239 Contact: Study Coordinator United States, Nevada Affiliated Clinical Research, Inc. Recruiting Las Vegas, Nevada, United States, 89113 Contact: Study Coordinator United States, New Jersey Center for Women's Health and Wellness Recruiting Plainsboro, New Jersey, United States, 08536 Contact: Study Coordinator United States, New Mexico Bosque Women Care/Cactus Clinical Research Recruiting Albuquerque, New Mexico, United States, 87109 Contact: Study Coordinator United States, North Carolina Carolina Women's Research and Wellness Center Recruiting Durham, North Carolina, United States, 27713 Contact: Study Coordinator United States, Ohio Aventiv Research, Inc. Recruiting Columbus, Ohio, United States, 43213 Contact: Study Coordinator United States, South Carolina Coastal Carolina Research Center, Inc. Recruiting Mount Pleasant, South Carolina, United States, 29464 Contact: Study Coordinator United States, Virginia University of Virginia Medical Park Northridge Recruiting Charlottesville, Virginia, United States, 22903 Contact: Study Coordinator United States, Washington Overlake Internal Medicine Associates, PS Recruiting Bellevue, Washington, United States, 98004 Contact: Study Coordinator Dedicated Women's Health Specialists Terminated Puyallup, Washington, United States, 98372 Germany Private Practice - Gynecology Not yet recruiting Frankfurt, Hessen, Germany, 60322 Contact: Study Coordinator Spain Instituto Palacios Salud de La Mujer Recruiting Madrid, Spain, 28009 Contact: Study Coordinator Collapse <<
NCT02067741	Metastatic Breast Adenocarcino... more >>ma Breast Cancer Collapse <<	Phase 2	Active, not recruiting	June 2027	Switzerland ... more >> Kantonsspital Aarau Aarau, Switzerland, CH-5001 Kantonsspital Baden Baden, Switzerland, CH-5404 Universitätsspital Basel Basel, Switzerland, CH-4031 Istituto Oncologico della Svizzera Italiana - Ospedale Regionale Bellinzona e Valli Bellinzona, Switzerland, CH-6500 Oncocare / Klinik Engeried Bern, Switzerland, 3012 Inselspital Bern Bern, Switzerland, CH-3010 Kantonsspital Graubünden Chur, Switzerland, CH-7000 Kantonsspital Frauenfeld / Brustzentrum Thurgau Frauenfeld, Switzerland, CH-8501 Luzerner Kantonsspital Luzern, Switzerland, CH-6000 Kantonsspital St. Gallen St. Gallen, Switzerland, CH-9007 Spital STS AG Thun, Switzerland, CH-3600 Kantonsspital Winterthur Winterthur, Switzerland, CH-8401 Onkozentrum - Klinik im Park Zurich, Switzerland, CH-8002 Collapse <<

4-羟基他莫昔芬 Catalog No. CSN22105

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