"目錄號: HY-13757A
Tamoxifen 是一種抗雌激素，抑制雌激素結(jié)合到雌激素受體 (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
University of Nottingham
Cancer-Gastrointestinal Neoplasms
December 2015
Phase 1
Roswell Park Cancer Institute-National Institutes of Health (NIH)-National Cancer Institute (NCI)
Breast Cancer
December 14, 2009
Bader, Ted, M.D.
Chronic Hepatitis C
November 2008
Phase 1
National Cancer Center, Korea
Breast Cancer-Metastatic Disease
June 2006
Phase 2
Dana-Farber Cancer Institute-Brigham and Women's Hospital-Massachusetts General Hospital-AstraZeneca
Hodgkin's Disease-Breast Cancer
April 2001
Baylor College of Medicine-National Cancer Institute (NCI)
Bladder Cancer
June 2015
Phase 2
Washington University School of Medicine
Barrett Metaplasia
July 9, 2014
Early Phase 1
Radboud University
Breast Cancer
July 2010
Phase 1
Oana Danciu, MD-Pfizer-Big Ten Cancer Research Consortium
Hormone Receptor Positive Malignant Neoplasm of Breast-Human Epidermal Growth Factor 2 Negative Carcinoma of Breast-Estrogen Receptor Positive Breast Cancer-Progesterone Receptor Positive Tumor-Metastatic Breast Cancer
June 2016
Phase 2
Seth Lerner-AstraZeneca-Cytogen Corporation-Baylor College of Medicine
Urinary Bladder Neoplasms
January 2007
Phase 2
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
Western Sydney Local Health District-St George Hospital, Australia
Breast Cancer-CYP2D6 Polymorphism
March 2010
Oregon Health and Science University
Menorrhagia-Metrorrhagia-Medicated Intrauterine Devices
September 2016
Phase 4
Austrian Breast & Colorectal Cancer Study Group
Early-stage Breast Cancer
December 1990
Phase 3
UNC Lineberger Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer-Menopausal Symptoms
June 2008
Phase 2
Baylor Breast Care Center-AstraZeneca
Breast Cancer
July 2003
Phase 2
Centre Francois Baclesse-National Cancer Institute, France-ARC Foundation for Cancer Research
Postmenopausal-Metastatic Breast Cancer
January 2015
Phase 2
Jenny C. Chang, MD-Millennium Pharmaceuticals, Inc.-The Methodist Hospital System
Estrogen Receptor Positive Breast Cancer
April 24, 2017
Phase 2
Nazem Atassi-ALS Therapy Alliance-State University of New York - Upstate Medical University-Massachusetts General Hospital
Amyotrophic Lateral Sclerosis
March 2011
Phase 2
National Cancer Center, Korea
Breast Cancer
August 2015
Oregon Health and Science University-Society of Family Planning
Menstruation Disturbances
February 2014
Phase 4
Pfizer
Pharmacokinetics
August 2010
Phase 4
Tata Memorial Hospital-Indian Council of Medical Research
Pulmonary Fibrosis-Breast Cancer
December 2008
Phase 3
Icahn School of Medicine at Mount Sinai
Breast Cancer
January 2009
Phase 4
Sidney Kimmel Comprehensive Cancer Center-Merck Sharp & Dohme Corp.
Stage I Breast Cancer-Stage II Breast Cancer-Stage III Breast Cancer-Invasive Breast Cancer
March 2011
Phase 2
Korea University Anam Hospital-National Cancer Center, Korea-Korean Breast Cancer Study Group
Breast Neoplasms-Tamoxifen-Genotype-CYP2D6
March 2009
Austrian Breast & Colorectal Cancer Study Group-AstraZeneca-Novartis Pharmaceuticals
Breast Cancer
June 1999
Phase 3
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
Icahn School of Medicine at Mount Sinai-AstraZeneca
Breast Cancer
October 2016
Phase 1
European Institute of Oncology
Breast Cancer
March 2002
Phase 3
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
Phase 2
Wake Forest University-National Institute on Aging (NIA)-Wake Forest University Health Sciences
Cognition-Aging
October 2001
Phase 3
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
Meningitis Streptococcal-Hiv-Meningitis-Meningoencephalitis
August 1, 2017
Phase 2
European Organisation for Research and Treatment of Cancer - EORTC
Breast Cancer
November 2006
Phase 1
The Netherlands Cancer Institute-Genentech, Inc.-EurocanPlatform-Rather
Breast Cancer-Ovarian Cancer-Cancer of the Uterus
November 2014
Phase 1
Vanderbilt University-Washington University School of Medicine-Instituto National de Cancerologia, Guatemala
Breast Cancer-Breast Neoplasms
January 2013
Phase 2
H. Lee Moffitt Cancer Center and Research Institute-Merck Sharp & Dohme Corp.
Breast Cancer
February 2006
Phase 2
Sun Yat-sen University
Breast Cancer Metastatic
February 1, 2017
Phase 2
AstraZeneca-Institute of Cancer Research, United Kingdom
Breast Cancer
March 1998
Phase 3
Korean Breast Cancer Study Group
Breast Cancer
May 2009
Phase 3
Shanghai Jiao Tong University School of Medicine
Breast Cancer
December 2014
Phase 4
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University-Sun Yat-sen University
Infertility
January 2017
Phase 4
Universidade Federal de Goias
Pain-Discomfort
July 2016
Phase 2-Phase 3
Centre Hospitalier Universitaire Vaudois
Breast Cancer
June 2009
Phase 3
Institut Claudius Regau
