"目录号: HY-13757A
OthersAutophagy-
Tamoxifen 是一种抗雌激素，抑制雌激素结合到雌激素受体 (estrogen receptors)。
Estrogen Receptor/ERRAutophagy
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生物活性
Description
Tamoxifen is an antiestrogen by inhibiting the binding of estrogen toestrogen receptors.
IC50& Target
Estrogen receptor[1]
In Vitro
Tamoxifen shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 cells[2].
In Vivo
The Tamoxifen-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1-/-mice are given a daily Iintraperitoneal injection of Tamoxifen at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen-inducible cardiac-specific disruption of Med1 (TmcsMed1-/-) in adult mice causes dilated cardiomyopathy[3].
Clinical Trial
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Cancer-Gastrointestinal Neoplasms
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Phase 1
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Roswell Park Cancer Institute-National Institutes of Health (NIH)-National Cancer Institute (NCI)
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Bader, Ted, M.D.
Chronic Hepatitis C
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National Cancer Center, Korea
Breast Cancer-Metastatic Disease
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Dana-Farber Cancer Institute-Brigham and Women's Hospital-Massachusetts General Hospital-AstraZeneca
Hodgkin's Disease-Breast Cancer
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Baylor College of Medicine-National Cancer Institute (NCI)
Bladder Cancer
June 2015
Phase 2
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Washington University School of Medicine
Barrett Metaplasia
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Radboud University
Breast Cancer
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Phase 1
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Oana Danciu, MD-Pfizer-Big Ten Cancer Research Consortium
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Seth Lerner-AstraZeneca-Cytogen Corporation-Baylor College of Medicine
Urinary Bladder Neoplasms
January 2007
Phase 2
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Taipei Medical University Shuang Ho Hospital
Amyotrophic Lateral Sclerosis-ALS Functional Ration Scale-TAR-DNA-binding Protein-43-Tamoxifen-mTOR
April 2014
Phase 1-Phase 2
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Western Sydney Local Health District-St George Hospital, Australia
Breast Cancer-CYP2D6 Polymorphism
March 2010
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Oregon Health and Science University
Menorrhagia-Metrorrhagia-Medicated Intrauterine Devices
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Phase 4
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Austrian Breast & Colorectal Cancer Study Group
Early-stage Breast Cancer
December 1990
Phase 3
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UNC Lineberger Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer-Menopausal Symptoms
June 2008
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Baylor Breast Care Center-AstraZeneca
Breast Cancer
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Centre Francois Baclesse-National Cancer Institute, France-ARC Foundation for Cancer Research
Postmenopausal-Metastatic Breast Cancer
January 2015
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Jenny C. Chang, MD-Millennium Pharmaceuticals, Inc.-The Methodist Hospital System
Estrogen Receptor Positive Breast Cancer
April 24, 2017
Phase 2
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Nazem Atassi-ALS Therapy Alliance-State University of New York - Upstate Medical University-Massachusetts General Hospital
Amyotrophic Lateral Sclerosis
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National Cancer Center, Korea
Breast Cancer
August 2015
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Oregon Health and Science University-Society of Family Planning
Menstruation Disturbances
February 2014
Phase 4
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Pfizer
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Icahn School of Medicine at Mount Sinai
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Breast Neoplasms-Tamoxifen-Genotype-CYP2D6
March 2009
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Austrian Breast & Colorectal Cancer Study Group-AstraZeneca-Novartis Pharmaceuticals
Breast Cancer
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Phase 3
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Buddhist Tzu Chi General Hospital-Chang Gung Memorial Hospital-Chung Shan Medical University-China Medical University Hospital-National Cheng-Kung University Hospital-Kaohsiung Medical University Chung-Ho Memorial Hospital-Kaohsiung Veterans General Hospital.-Taiwan Ministry of Science and Technology
Uterine Cervical Neoplasms
May 2015
Phase 2
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Icahn School of Medicine at Mount Sinai-AstraZeneca
Breast Cancer
October 2016
Phase 1
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European Institute of Oncology
Breast Cancer
March 2002
Phase 3
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University of Alabama at Birmingham-National Cancer Institute (NCI)-St. Jude Children's Research Hospital-University Health Network, Toronto-University of Michigan-Dana-Farber Cancer Institute-Mayo Clinic-University of Washington-City of Hope National Medical Center-M.D. Anderson Cancer Center-University of Chicago-University of Minnesota - Clinical and Translational Science Institute-University of Colorado, Denver-Wake Forest University
Breast Cancer
September 2010
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Wake Forest University-National Institute on Aging (NIA)-Wake Forest University Health Sciences
Cognition-Aging
October 2001
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Oxford University Clinical Research Unit, Vietnam-Hospital for Tropical Diseases, Ho Chi Minh City, Vietnam-Cho Ray Hospital, Ho Chi Minh City, Vietnam-University of Liverpool-University of Rochester-Liverpool School of Tropical Medicine
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August 1, 2017
Phase 2
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European Organisation for Research and Treatment of Cancer - EORTC
Breast Cancer
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The Netherlands Cancer Institute-Genentech, Inc.-EurocanPlatform-Rather
Breast Cancer-Ovarian Cancer-Cancer of the Uterus
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Vanderbilt University-Washington University School of Medicine-Instituto National de Cancerologia, Guatemala
Breast Cancer-Breast Neoplasms
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H. Lee Moffitt Cancer Center and Research Institute-Merck Sharp & Dohme Corp.
Breast Cancer
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Phase 2
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Sun Yat-sen University
Breast Cancer Metastatic
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AstraZeneca-Institute of Cancer Research, United Kingdom
Breast Cancer
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Phase 3
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Korean Breast Cancer Study Group
Breast Cancer
May 2009
Phase 3
NCT02344940
Shanghai Jiao Tong University School of Medicine
Breast Cancer
December 2014
Phase 4
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Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University-Sun Yat-sen University
Infertility
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Universidade Federal de Goias
Pain-Discomfort
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Centre Hospitalier Universitaire Vaudois
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Institut Claudius Regau