"目录号: HY-14274
Anastrozole 是一种选择性的芳香酶 (aromatase) 抑制剂，抑制胎盘芳香化酶，IC50为 15 nM。
相关产品
Letrozole-Testolactone-Exemestane-Formestane-Aminoglutethimide-4-Hydroxytestosterone-Fadrozole-Org30958-
生物活性
Description
Anastrozole is a potent, highly selectivearomataseinhibitor, which inhibits human placental aromatase with anIC50of 15 nM.
IC50& Target
IC50: 15 nM (human aromatase)[1]
In Vitro
Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental aromatase with an IC50of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide (AG), twice as potent as 4-OHA and one third as potent as Fadrozole[1].
In Vivo
Groups of eight immature (22-day-old) female rats are given androstenedione (AD) (30 mg/kg) in arachis oil s.c. daily for3 days with or without various doses of Anastrozole p.o. on day 4 the uteri are dissected, blotted and weighed. An oral dose of 0.1 mg/kg of Anastrozole given on day 2 or day 3 of the cycle completely blocked ovulation. At the same daily dosage (0.1 mg/kg), Anastrozole completely extinguished the uterotrophic activity of exogenous AD in immature rats. In male pigtailed monkeys, twice-daily oral treatment with 0.1 mg/kg and above of Anastrozole reduced circulating oestradiol concentrations by 50-60%[1].
Clinical Trial
University of Pennsylvania-National Heart, Lung, and Blood Institute (NHLBI)-Johns Hopkins University-University of Colorado, Denver-Rhode Island Hospital-Stanford University-Vanderbilt University-Washington University School of Medicine
Pulmonary Arterial Hypertension
September 2017
Phase 2
Maastricht University Medical Center
Breast Cancer
June 2006
Phase 3
AstraZeneca
Breast Cancer
May 2005
Dr. Reddy's Laboratories Limited
Healthy
May 2008
Phase 1
Dr. Reddy's Laboratories Limited
Healthy
May 2008
Phase 1
Teva Pharmaceuticals USA
Healthy
September 2005
Phase 1
Teva Pharmaceuticals USA
Healthy
August 2005
Phase 1
Hamilton Health Sciences Corporation-Canadian Institutes of Health Research (CIHR)-McMaster University
Breast Cancer
January 2007
Fudan University
Carcinoma Breast Stage IV
March 2014
Phase 2
Sidney Kimmel Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer
January 2004
Phase 2
AstraZeneca
Breast Cancer
January 2004
Phase 2
AstraZeneca-Institute of Cancer Research, United Kingdom
Breast Cancer
March 1998
Phase 3
AstraZeneca
Breast Cancer
March 1, 2004
Phase 3
ArQule
Solid Tumors-Ovarian Cancer-Endometrial Cancer
June 2015
Phase 1
AstraZeneca-Aardex Pharmionic
Breast Cancer
June 2009
Ottawa Hospital Research Institute-Canadian Breast Cancer Foundation
Breast Cancer
October 2012
Phase 2
Massachusetts General Hospital-National Institute on Aging (NIA)
Hypogonadism
October 2004
Phase 2
Trans-Tasman Radiation Oncology Group (TROG)
Breast Cancer
September 2009
Phase 3
Hospital Affiliated to Military Medical Science, Beijing
Metastatic Breast Cancer
January 2014
Phase 2
Stanford University-AstraZeneca
Breast Cancer
January 2008
Phase 2
Centre Leon Berard
Endometrial Carcinoma-Metastatic Carcinoma-Hormone Receptor Positive Tumor
April 2016
Phase 1-Phase 2
AstraZeneca
Neoplasms-Breast Neoplasms-Breast Cancer
June 2010
Phase 2
Austrian Breast & Colorectal Cancer Study Group-AstraZeneca-Novartis Pharmaceuticals
Breast Cancer
June 1999
Phase 3
AstraZeneca
Puberty, Precocious
November 22, 2004
Phase 2
University of Pennsylvania
Pulmonary Arterial Hypertension
October 2012
Phase 2
AstraZeneca
Safety-Pharmacokinetics
April 2012
Phase 1
Antoinette Tan-Pfizer-Carolinas Healthcare System
Female Breast Carcinoma
November 2016
Phase 2
Queen Mary University of London
Breast Cancer
September 2003
Phase 3
Federal University of São Paulo
Breast Cancer
April 2005
University of California, Irvine-AstraZeneca
DCIS
September 2004
Phase 2
Joyce Marie Slingerland-Stanford University-University of Miami
Breast Cancer
October 2008
Phase 1-Phase 2
Sidney Kimmel Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer
June 2006
Phase 2
Roxane Laboratories
Breast Cancer
May 2006
Roxane Laboratories
Breast Cancer
April 2006
University of Maryland-Syndax Pharmaceuticals
Estrogen Receptor-negative Breast Cancer-HER2-negative Breast Cancer-Progesterone Receptor-negative Breast Cancer-Stage I Breast Cancer-Stage II Breast Cancer-Stage IIIA Breast Cancer-Triple-negative Breast Cancer
October 2010
Phase 2
AstraZeneca
Early Breast Cancer
June 2006
Phase 4
Merck Sharp & Dohme Corp.
Breast Cancer
December 2003
Phase 2
SCRI Development Innovations, LLC-Genentech, Inc.-AstraZeneca
Breast Cancer-Breast Neoplasms
November 2006
Phase 2
Queen Mary University of London-Cancer Research UK
Breast Cancer
September 2003
Phase 3
AstraZeneca
Breast Cancer
April 2006
Phase 2
Massachusetts General Hospital-Dana-Farber Cancer Institute-Brigham and Women's Hospital
Ovarian Cancer-Peritoneal Carcinoma-Tubal Carcinoma
October 2003
Phase 2
AstraZeneca-German Adjuvant Breast Cancer Group
Breast Cancer
November 1996
Phase 2
AstraZeneca
Breast Cancer
April 2004
Phase 4
AstraZeneca
Breast Cancer
January 2004
Phase 3
Imperial College London-Cancer Research UK-AstraZeneca
Breast Cancer
July 2012
Phase 1-Phase 2
National Cancer Institute (NCI)
Recurrent Breast Cancer-Stage IV Breast Cancer
June 2005
Phase 1-Phase 2
Stanford University
Short Stature
November 2009
Phase 4
European Organisation for Research and Treatment of Cancer - EORTC
Breast Cancer
May 2003
Phase 2
University of Arizona-National Cancer Institute (NCI)-GlaxoSmithKline
Estrogen Receptor-positive Breast Cancer-Human Epidermal Growth Factor 2 Negative Carcinoma of Breast-Male Breast Cancer-Recurrent Breast Cancer-Stage II Breast Cancer-Stage IIIA Breast Cancer-Stage IIIB Breast Cancer
July 13, 2011
