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Chemical Structure| 90357-06-5 Chemical Structure| 90357-06-5
Chemical Structure| 90357-06-5

Bicalutamide

CAS No.: 90357-06-5

Bicalutamide is an orally active, non-steroidal androgen receptor (AR) antagonist used in prostate cancer research.

Synonyms: ICI 176334; ZD 176334; Abbreviation

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Cat. No.: A176397 Purity: 99%

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Product Details of Bicalutamide

CAS No. :90357-06-5
Formula : C18H14F4N2O4S
M.W : 430.37
SMILES Code : O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)C(C)(O)CS(=O)(C2=CC=C(F)C=C2)=O
Synonyms :
ICI 176334; ZD 176334; Abbreviation
MDL No. :MFCD00869971
InChI Key :LKJPYSCBVHEWIU-UHFFFAOYSA-N
Pubchem ID :2375

Safety of Bicalutamide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Androgen Receptor

    Androgen Receptor, IC50:0.16 μM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
PC3 30 μM 48 h Bicalutamide inhibited the growth of PC3 cells, and a significant inhibition of cell growth was observed when combined with Curcumin. PMC4446835
DU145 30 μM 48 h Bicalutamide inhibited the growth of DU145 cells, and a significant inhibition of cell growth was observed when combined with Curcumin. PMC4446835
LNCaP 30 μM 48 h Bicalutamide inhibited the growth of LNCaP cells, and a significant inhibition of cell growth was observed when combined with Curcumin. PMC4446835
Rat mesangial cells (RMC) 30 μM and 60 μM 24 hours Bicalutamide enhanced lactate dehydrogenase release, reactive oxygen species (ROS) production, lysosome population, and kidney injury molecule-1, and decreased N-cadherin. Bicalutamide elicited mitochondrial swelling and reduced the mitochondrial potential, resulting in severe suppression of the oxygen consumption rate (OCR), maximum respiration, and ATP production. PMC7247665
LNCaP cells 1.0 µM 12 days SPH potentiated the anti-proliferative effect of Bicalutamide on LNCaP cells, with relative colony survival decreasing from 25% to 2% in the presence of 160 µg/mL SPH and 1.0 µM Bicalutamide. PMC9032914
PC3 cells 10.0 µM 12 days SPH potentiated the anti-proliferative effect of Bicalutamide on PC3 cells, with relative colony survival decreasing from 52% to 32% in the presence of 160 µg/mL SPH and 10.0 µM Bicalutamide. PMC9032914
LNCaP cells 1 µM - 40 µM 12 months Generated bicalutamide resistant LNCaP cells (LNCaP-BicR) and found that these resistant cells express significantly increased levels of AR variants, particularly AR-V7, both at the mRNA and protein levels. PMC5544572
CWR22Rv1 cells 20 µM 3 and 5 days Niclosamide and bicalutamide combination treatment significantly suppressed the growth of CWR22Rv1 cells and induced apoptosis. PMC5544572
C4-2B MDVR cells 20 µM 3 and 5 days Niclosamide and bicalutamide combination treatment significantly suppressed the growth of C4-2B MDVR cells and induced apoptosis. PMC5544572
LNCaP cells 30 µM 7 days Investigated the effect of Bicalutamide on LNCaP cells, finding that Bicalutamide increased the expression of ERα and NRF2, and decreased the expression of AR. PMC9661764
IPC-366 100 nM 24 hours To evaluate the effect of bicalutamide combined with docetaxel on cell proliferation and migration. Results showed that the combination of bicalutamide and docetaxel significantly reduced proliferation and migration in IPC-366 cells. PMC11276844
SUM149 100 nM 24 hours To evaluate the effect of bicalutamide combined with docetaxel on cell proliferation and migration. Results showed that the combination of bicalutamide and docetaxel significantly reduced proliferation and migration in SUM149 cells. PMC11276844

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
SCID mice CWR22Rv1 xenograft model Oral (p.o) 1.5 mg/kg Single injection, observed for 6 days Niclosamide and bicalutamide combination treatment significantly suppressed the growth of CWR22Rv1 xenografts, indicating that the combination therapy can overcome enzalutamide resistance. PMC5544572
Mice KI AR113Q mouse model Subcutaneous injection 20 mg/kg Single dose 2 hours before, lasting for 14 days Bicalutamide and trehalose ameliorated SBMA pathology, extended the survival of mice, improved motor behavior, and partially recovered muscle morphology. Bicalutamide also prevented the formation of AR insoluble forms and possibly restored the autophagic flux. PMC10121997
Balb/SCID mice IPC-366 and SUM149 cell xenograft model Bicalutamide: drinking water; Docetaxel and Doxorubicin: intraperitoneal injection 25 mg/kg 3 weeks To evaluate the effect of bicalutamide combined with docetaxel and doxorubicin on tumor growth. Results showed that the triple combination significantly reduced tumor volume in IPC-366 and SUM149 mice. PMC11276844

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00298155 Cancer Prosta... More >>te Neoplasms Less << Phase 2 Completed - United States, Washington ... More >> Veterans' Administration Puget Sound Health Care System (VAPSHCS) Seattle, Washington, United States, 98108-1532 University of Washington Seattle, Washington, United States, 98195-6158 Less <<
NCT00298155 - Completed - -
NCT02064036 Adenocarcinoma of the Prostate Not Applicable Recruiting October 2018 United States, California ... More >> UC Davis Sacramento Cancer Center Dept of Radiation Oncology Recruiting Sacramento, California, United States, 95817 Contact: Richard Valicenti, MD    916-724-8295    rkvalicenti@ucdavis.edu    Principal Investigator: Richard Valicenti, MD Less <<
NCT00567580 Prostate Cancer Phase 3 Active, not recruiting December 2025 -
NCT00769795 Prostate Cancer Phase 2 Completed - United States, Washington ... More >> Virginia Mason Medical Center Seattle, Washington, United States, 98101 Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 University of Washington Medical Center Seattle, Washington, United States, 98195 Less <<
NCT02346578 Castration-resistant Prostate ... More >>Cancer Less << Phase 2 Active, not recruiting March 2020 Japan ... More >> Osaka City University Graduate School of Medicine Osaka, Japan Less <<
NCT01120262 - Completed - -
NCT02615223 Stage IV Prostate Cancer Not Applicable Unknown December 2018 China, Tianjin ... More >> Tianjin Medical University Cancer Institute and Hospital Recruiting Tianjin, Tianjin, China, 300060 Contact: Zhi Guo, PhD    02223340123 ext 1095    cjr.guozhi@vip.163.com    Contact: Tongguo Si, PhD    02223340123 ext 1095    sitg77@163.com Less <<
NCT00004124 - Active, not recruiting - -
NCT03119857 Prostatic Neoplasms Phase 3 Active, not recruiting December 2023 Denmark ... More >> Copenhagen University hospital, Rigshospitalet Copenhagen, Denmark Finland Kuopio University Hospital Kuopio, Kuopio Kuopio, Finland, 70211 Turku University Hospital Turku, Finland, 20521 Netherlands Erasmus Medical Center Rotterdam Rotterdam, Netherlands, 3015 CE Sweden Sahlgrenska University Hospital Göteborg, Sweden, 41345 Less <<
NCT00536653 Osteoporosis Not Applicable Completed - United Kingdom ... More >> Wirral University Hospitals NHS Trust Upton, Wirral, Merseyside, United Kingdom, CH48 5PE Less <<
NCT00514917 Prostatic Neoplasms Phase 3 Terminated(Company decision to... More >> discontinue the study, not due to any safety or efficacy concerns) Less << - United States, New Jersey ... More >> Sanofi-Aventis Administrative Office Bridgewater, New Jersey, United States, 08807 Belgium Sanofi-Aventis Administrative Office Diegem, Belgium Canada Sanofi-Aventis Administrative Office Laval, Canada Czech Republic Sanofi-Aventis Administrative Office Praha, Czech Republic Germany Sanofi-Aventis Administrative Office Frankfurt, Germany Lithuania Sanofi-Aventis Administrative Office Vilnius, Lithuania Poland Sanofi-Aventis Administrative Office Warsaw, Poland Slovakia Sanofi-Aventis Administrative Office Bratislava, Slovakia Spain Sanofi-Aventis Administrative Office Barcelona, Spain Less <<
NCT00514917 - Terminated(Company decision to... More >> discontinue the study, not due to any safety or efficacy concerns) Less << - -
NCT01342367 Prostate Cancer Not Applicable Recruiting April 2019 United States, Illinois ... More >> University of Chicago Recruiting Chicago, Illinois, United States, 60637 Contact: Fauzia Arif       farif@radonc.uchicago.edu Less <<
NCT02716974 Prostate Cancer Phase 2 Recruiting March 2021 United States, District of Col... More >>umbia Sibley Memorial Hospital Recruiting Washington, District of Columbia, United States, 20016 Contact: Channing Paller, MD    202-660-6500    cpaller1@jhmi.edu    United States, Maryland Johns Hopkins School of Medicine - Sidney Kimmel Comprehensive Cancer Center Recruiting Baltimore, Maryland, United States, 21205 Johns Hopkins Bayview Medical Center Recruiting Baltimore, Maryland, United States, 21224 Contact: Christian Pavlovich, MD    410-550-3338    cpavlov2@jhmi.edu Less <<
NCT00666666 Adenocarcinoma of the Prostate... More >> Stage IV Prostate Cancer Less << Phase 2 Completed - United States, Illinois ... More >> University of Chicago Chicago, Illinois, United States, 60637 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, New Jersey Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Less <<
NCT02918968 Prostate Cancer Phase 4 Active, not recruiting March 2020 Japan ... More >> Site JP00024 Aichi, Japan Site JP00025 Aichi, Japan Site JP00010 Chiba, Japan Site JP00053 Chiba, Japan Site JP00038 Ehime, Japan Site JP00039 Fukuoka, Japan Site JP00040 Fukuoka, Japan Site JP00050 Fukuoka, Japan Site JP00051 Fukuoka, Japan Site JP00005 Gunma, Japan Site JP00043 Gunma, Japan Site JP00045 Gunma, Japan Site JP00035 Hiroshima, Japan Site JP00001 Hokkaido, Japan Site JP00002 Hokkaido, Japan Site JP00048 Hokkaido, Japan Site JP00054 Hokkaido, Japan Site JP00055 Ibaraki, Japan Site JP00019 Kanagawa, Japan Site JP00020 Kanagawa, Japan Site JP00021 Kanagawa, Japan Site JP00044 Kanagawa, Japan Site JP00026 Kyoto, Japan Site JP00006 Nagano, Japan Site JP00008 Nagano, Japan Site JP00041 Nagasaki, Japan Site JP00046 Nara, Japan Site JP00033 Okayama, Japan Site JP00027 Osaka, Japan Site JP00028 Osaka, Japan Site JP00029 Osaka, Japan Site JP00030 Osaka, Japan Site JP00031 Osaka, Japan Site JP00032 Osaka, Japan Site JP00042 Saga, Japan Site JP00009 Saitama, Japan Site JP00022 Shizuoka, Japan Site JP00049 Tochigi, Japan Site JP00037 Tokushima, Japan Site JP00011 Tokyo, Japan Site JP00013 Tokyo, Japan Site JP00014 Tokyo, Japan Site JP00016 Tokyo, Japan Site JP00017 Tokyo, Japan Site JP00018 Tokyo, Japan Site JP00052 Toyama, Japan Site JP00034 Yamaguchi, Japan Less <<
NCT00666666 - Completed - -
NCT01642732 Prostate Cancer Phase 1 Terminated(Lack of accrual and... More >> funding expires in June, 2014.) Less << - United States, District of Col... More >>umbia Georgetown University Washington, D.C., District of Columbia, United States, 20057 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109 Less <<
NCT01642732 - Terminated(Lack of accrual and... More >> funding expires in June, 2014.) Less << - -
NCT00702923 Prostate Cancer Phase 1 Terminated(Enrollment was halt... More >>ed prematurely due to slow accrual.) Less << - United States, Wisconsin ... More >> University of Wisconsin Paul P. Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Less <<
NCT00684905 Prostate Cancer Phase 2 Completed - United States, Arizona ... More >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 Less <<
NCT00943956 Prostate Cancer Phase 1 Completed - France ... More >> Centre Regional de Lutte Contre le Cancer - Centre Val d'Aurelle Montpellier, France, 34298 Less <<
NCT00021450 Prostate Cancer Phase 3 Completed - Belgium ... More >> Academisch Ziekenhuis der Vrije Universiteit Brussel Brussels, Belgium, 1090 Cliniques Universitaires Saint-Luc Brussels, Belgium, 1200 U.Z. Gasthuisberg Leuven, Belgium, B-3000 Cyprus Bank Of Cyprus Oncology Centre Nicosia, Cyprus, 2006 Strovolos Czech Republic Charles University Hospital Hradec Kralove, Czech Republic, 500 05 France Centre Hospitalier Regional de Besancon - Hopital Jean Minjoz Besancon, France, 25030 Centre de Lutte Contre le Cancer Georges-Francois Leclerc Dijon, France, 21079 CHU de Grenoble - Hopital de la Tronche Grenoble, France, 38043 Centre Paul Strauss Strasbourg, France, 67085 Centre d'Oncologie Saint-Yves Vannes, France, 56001 Ireland Saint Luke's Hospital Dublin, Ireland, 6 Italy Spedali Civili di Brescia Brescia, Italy, 25124 Istituto Nazionale per la Ricerca sul Cancro Genoa, Italy, 16132 Luxembourg Hopital de la Ville D'Esch-sur-Alzette Esch-sur-Alzette, Luxembourg, L-4240 Netherlands Arnhems Radiotherapeutisch Instituut Arnhem, Netherlands, 6815 AD University Medical Center Groningen Groningen, Netherlands, 9700 RB Dr. Bernard Verbeeten Instituut Tilburg, Netherlands, 5042 SB Poland Medical University of Gdansk Gdansk, Poland, 80-211 Spain Institut Catala d'Oncologia - Hospital Duran i Reynals Barcelona, Spain, 08907 United Kingdom Belfast City Hospital Trust Incorporating Belvoir Park Hospital Belfast, Northern Ireland, United Kingdom, BT8 8JR Less <<
NCT00004124 Prostate Cancer Phase 3 Active, not recruiting June 1, 2022 -
NCT00349557 Prostate Cancer Phase 2 Completed - United States, Washington ... More >> Virginia Mason Medical Center Seattle, Washington, United States, 98101 Less <<
NCT00067015 Prostate Cancer Phase 3 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less <<
NCT00014586 Prostate Cancer Phase 3 Terminated(low accrual) - Germany ... More >> Center of Operative Urology Bremen Bremen, Germany, D-28277 Less <<
NCT00702923 - Terminated(Enrollment was halt... More >>ed prematurely due to slow accrual.) Less << - -
NCT01415778 Healthy Phase 1 Completed - -
NCT02085252 Prostate Cancer Phase 3 Completed - France ... More >> Tenon Hospital Paris France Paris, France, 75020 Ouzid, Paris La Défense, Paris, France, 92977 Less <<
NCT00924807 Prostate Cancer Phase 1 Phase 2 Terminated(Sponsor closed the ... More >>trial) Less << - United States, New York ... More >> St.Luke's-Roosevelt Hospital Center New York, New York, United States, 10019 Less <<
NCT00319787 Locally Advanced Prostate Canc... More >>er Less << Phase 2 Completed - Norway ... More >> Research Site Moelv, Norway Research Site Oslo, Norway Research Site Trondheim, Norway Less <<
NCT00255268 Metastatic Prostate Cancer Phase 4 Withdrawn - Mexico ... More >> Research Site Metepec, Mexico Research Site Mexico City, Mexico Less <<
NCT01020305 Prostate Cancer ... More >> Prostatic Neoplasms Castrate-resistant Prostate Cancer (CRPC) Androgen-insensitive Prostate Cancer Hormone-refractory Prostate Cancer Metastatic Disease Less << Phase 1 Phase 2 Terminated(Decision by funding... More >> sponsor due to poor accrual) Less << - United States, California ... More >> Stanford University School of Medicine Stanford, California, United States, 94305 Less <<
NCT02582749 Prostate Cancer ... More >> Bone Metastases Prostate Neoplasms Less << Phase 2 Active, not recruiting January 2020 United States, Arizona ... More >> University of Arizona Cancer Center at Dignity Health St. Joseph's Phoenix, Arizona, United States, 85004 United States, Illinois Illinois CancerCare, P. C. Peoria, Illinois, United States, 61615 United States, Indiana Indiana University Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202 IU Health Central Indiana Cancer Centers Indianapolis, Indiana, United States, 46219 United States, Iowa University of Iowa Hopital and Clinics Iowa City, Iowa, United States, 52242 United States, Michigan University of Michigan Health System Ann Arbor, Michigan, United States, 48109 Henry Ford Hospital Detroit, Michigan, United States, 48202 Metro Health Cancer Center Wyoming, Michigan, United States, 49519 United States, Nebraska GU Research Network, LLC Omaha, Nebraska, United States, 68130 United States, New York Integrated Medical Professionals, PLLC Lake Success, New York, United States, 11042 United States, Texas University of Texas Medical Branch at Galveston Galveston, Texas, United States, 77555 United States, Wisconsin Clement J. Zablocki VA Medical Center Milwaukee, Wisconsin, United States, 53295 Less <<
NCT01020305 - Terminated(Decision by funding... More >> sponsor due to poor accrual) Less << - -
NCT00470834 Neoplasms, Prostate Phase 4 Completed - -
NCT00470834 - Completed - -
NCT00919477 - Completed - -
NCT01120236 Prostate Adenocarcinoma ... More >> Recurrent Prostate Carcinoma Stage IV Prostate Cancer Less << Phase 2 Completed - -
NCT01120236 - Completed - -
NCT00188708 Prostatic Neoplasms Phase 2 Active, not recruiting April 2019 Canada, Ontario ... More >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00924807 - Terminated(Sponsor closed the ... More >>trial) Less << - -
NCT00688532 - Completed - -
NCT00421694 Prostate Cancer PHASE2|PHASE3 COMPLETED - University of L'Aquila, L'Aqui... More >>la, Abruzzo, 67100, Italy Less <<
NCT00418080 Prostate Cancer Phase 2 Completed - Italy ... More >> University of L'Aquila L'Aquila, Abruzzo, Italy, 67100 Less <<
NCT00293696 Prostate Cancer Phase 4 Completed - Finland ... More >> TUCH Tampere, Finland, 33521 Less <<
NCT02382094 Prostate Cancer PHASE3 COMPLETED 2025-07-12 -
NCT00233610 Prostate Cancer Phase 3 Completed - Italy ... More >> Research Site Bari, BA, Italy Research Site Bologna, BO, Italy Research Site Catania, CT, Italy Research Site Bagno a Ripoli, FI, Italy Research Site Firenze, FI, Italy Research Site Genova, GE, Italy Research Site Pisa, PI, Italy Research Site Parma, PR, Italy Research Site Udine, UD, Italy Research Site Como, Italy Research Site Roma, Italy Less <<
NCT00637871 Gynaecomastia ... More >> Prostate Cancer Less << Phase 2 Completed - -
NCT03358563 Prostate Cancer Early Phase 1 Recruiting January 2020 United States, Wisconsin ... More >> University of Wisconsin Carbone Cancer Center Recruiting Madison, Wisconsin, United States, 53792 Contact: Cancer Connect    800-622-8922    cancerconnect@uwcarbone.wisc.edu    Principal Investigator: Christos Kyriakopoulos, MD Less <<
NCT00672282 Non-Metastatic Prostate Cancer Phase 3 Completed - -
NCT00430235 Adenocarcinoma of the Prostate Phase 2 Completed - Canada, British Columbia ... More >> BC Cancer Agency - Vancouver Centre Vancouver, British Columbia, Canada, V5Z 4E6 Less <<
NCT00833248 Prostate Cancer Phase 3 Completed - -
NCT00086736 Prostate Cancer Phase 2 Completed - United States, Alabama ... More >> University of Alabama at Birmingham Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3300 Less <<
NCT00659438 Prostate Cancer Phase 2 Completed - France ... More >> Research Site Bordeaux Cedex, France Research Site Creteil, France Research Site Paris, France Research Site Reims Cedex, France Research Site Villejuif, France Less <<
NCT00659438 - Completed - -
NCT00884273 - Completed - -
NCT00012090 Fallopian Tube Cancer ... More >> Ovarian Cancer Primary Peritoneal Cavity Cancer Less << Phase 2 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less <<
NCT00831233 Prostate Cancer Phase 3 Terminated(Poor recruitment du... More >>e to rare targeted population) Less << - Germany ... More >> Facharztpraxis für Urologie Bamberg, Germany, 96047 Gemeinschaftspraxis Borken, Germany, 46325 Universitätsklinikum Dresden Dresden, Germany, 01307 Euromed Clinic Fürth, Germany, 90763 Urologische Gemeinschaftspraxis Hamburg, Germany, 22399 Gemeinschaftspraxis Köln, Germany, 50667 VITURO Gesellschaft für Klinische Studien Leipzig, Germany, 04109 Klinikum Offenbach GmbH Offenbach, Germany, 63069 Urologische Klinik Planegg Planegg, Germany, 82152 Wuppertaler Gemeinschaftspraxis Wuppertal, Germany, 42103 Spain Hospital Universitario Principe de Asturias Alcalá de Henares-Madrid, Spain, 28805 Fundacion Hospital Alcorcón Alcorcon, Spain, 28922 Fundación Puigvert Barcelona, Spain, 08025 Hospital de Basurto Bilbao (Bizkaia), Spain, 48013 Complejo Hospitalario Universitario A Coruña Coruña, Spain Hospital universitario Ramón y Cajal Madrid, Spain, 28034 Hospital Clinico Universitario S. Carlos Madrid, Spain, 28040 Hospital Universitario Puerta de Hierro Majadahonda, Madrid, Spain, 28222 Hospital Manacor Manacor, Spain, 07500 Hospital Universitario Central de Asturias Oviedo, Spain, 33006 Hospital Santiago de Compostela Santiago de Compostela, Spain, 15706 Hospital Virgen Macarena Sevilla, Spain, 41014 Hospital Xeral de Vigo Vigo, Spain, 36204 United Kingdom United Bristol Healthcare NHSTrust Bristol Royal Infirmary Bristol, United Kingdom, BS2 8HW Falkirk and District Royal Infirmary Falkirk, United Kingdom, FK1 5QE Southern General Hospital Glasgow, United Kingdom, G51 4TF Castle Hill Hospital Hull, United Kingdom, HU16 5JQ Whipps Cross University Hospital London, United Kingdom, E11 1NR The Royal Free Hospital London, United Kingdom, NW3 2QG King's College Hospital London, United Kingdom, SE5 9RS Derriford Hospital Plymouth, United Kingdom, PL6 8DH Royal Hallamshire Hospital, Sheffield South Sheffield, United Kingdom, S10 2JF Sunderland Royal Hospital Sunderland, United Kingdom, SR4 7TP Less <<
NCT00777959 Prostate Cancer Phase 2 Completed - -
NCT01658527 Prostate Cancer Phase 2 Withdrawn(Pharmaceutical compa... More >>ny has terminated orteronel (TAK-700) development for Prostate Cancer) Less << January 2017 Belgium ... More >> Onze Lieve Vrouw Ziekenhuis Aals, Belgium Cliniques Universitaires Saint-Luc Brussels, Belgium AZ Groeninge Kortrijk - Campus Vercruysselaan Kortrijck, Belgium CHU Dinant Godinne - UCL Namur Yvoir, Belgium Less <<
NCT00554086 Prostate Cancer Phase 2 Completed - Canada, Ontario ... More >> Sunnybrook Health Sciences Centre Toronto, Ontario, Canada, M4N 3M5 Less <<
NCT00590213 Prostate Cancer Phase 4 Completed - Turkey ... More >> Research Site Adana, Turkey Research Site Ankara, Turkey Research Site Diyarbak?r, Turkey Research Site Edirne, Turkey Research Site Eskisehir, Turkey Research Site Istanbul, Turkey Research Site Izmir, Turkey Research Site Manisa, Turkey Research Site Samsun, Turkey Less <<
NCT00831233 - Terminated(Poor recruitment du... More >>e to rare targeted population) Less << - -
NCT03520478 Prostate Cancer ... More >> Hormone-Dependent Prostate Cancer Less << Phase 3 Recruiting April 30, 2025 China ... More >> Ye Dingwei Recruiting Shanghai, China Contact: Dingwei Ye, Doctor Less <<
NCT00878436 Prostate Cancer ... More >> Prostatic Neoplasms Less << Phase 1 Phase 2 Completed - United States, New Jersey ... More >> The Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 United States, New York North Shore University Hospital-Monter Cancer Center Lake Success, New York, United States, 11042 NYU Cancer Center New York, New York, United States, 10016 United States, Oregon Oregon Health & Science University Portland, Oregon, United States, 97239 Less <<
NCT00833248 - Completed - -
NCT01416883 Healthy Phase 1 Terminated - -
NCT00841113 Prostate Cancer Phase 3 Completed - -
NCT00673205 Non-Metastatic Prostate Cancer Phase 3 Completed - -
NCT02058706 Adenocarcinoma of the Prostate... More >> Recurrent Prostate Cancer Stage IV Prostate Cancer Less << Phase 2 Active, not recruiting December 31, 2018 United States, Alabama ... More >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, Michigan Barbara Ann Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, Ohio Ohio State University Medical Center Columbus, Ohio, United States, 43210 Less <<
NCT00636259 - - - -
NCT00878436 - Completed - -
NCT00486642 Hormone-Resistant Prostate Can... More >>cer Recurrent Prostate Carcinoma Less << Phase 2 Completed - Canada, British Columbia ... More >> BCCA-Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Juravinski Cancer Centre at Hamilton Health Sciences Hamilton, Ontario, Canada, L8V 5C2 Cancer Centre of Southeastern Ontario at Kingston General Hospital Kingston, Ontario, Canada, K7L 5P9 London Regional Cancer Program London, Ontario, Canada, N6A 4L6 Ottawa Hospital and Cancer Center-General Campus Ottawa, Ontario, Canada, K1H 8L6 University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00685633 Prostate Cancer Phase 2 Withdrawn - -
NCT00486642 - Completed - -
NCT00959335 Prostate Cancer ... More >> Hirsutism Less << Phase 1 Completed - -
NCT01050842 Prostate Cancer ... More >> Adenocarcinoma of the Prostate Hormone-resistant Prostate Cancer Stage IV Prostate Cancer Less << Early Phase 1 Completed - United States, Arizona ... More >> Mayo Clinic In Arizona Scottsdale, Arizona, United States, 85259 Less <<
NCT00031889 Prostate Cancer Phase 2 Completed - Switzerland ... More >> Kantonspital Aarau Aarau, Switzerland, 5001 University Hospital Basel, Switzerland, CH-4031 Inselspital, Bern Bern, Switzerland, CH-3010 Spitalzentrum Biel Biel, Switzerland, CH-2500 Kantonsspital Bruderholz Bruderholz, Switzerland, CH-4101 Ratisches Kantons und Regionalspital Chur, Switzerland, CH-7000 Clinique De Genolier Genolier, Switzerland, Ch-1272 Centre Hospitalier Universitaire Vaudois Lausanne, Switzerland, CH-1011 Istituto Oncologico della Svizzera Italiana Lugano, Switzerland, CH-6900 Ospedale Beata Vergine Mendrisio, Switzerland, CH-6850 Institut Central des Hopitaux Valaisans Sion, Switzerland, CH1951 Universitaetsspital Zurich, Switzerland, CH-8091 Less <<
NCT01200810 Adenocarcinoma of the Prostate... More >> Recurrent Prostate Cancer Stage IV Prostate Cancer Less << Phase 2 Terminated(Drug was no longer ... More >>available) Less << - United States, New Jersey ... More >> Rutgers Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 Less <<
NCT00884273 Prostate Cancer Phase 3 Completed - -
NCT00002874 Prostate Cancer Phase 3 Active, not recruiting - -
NCT01200810 - Terminated(Drug was no longer ... More >>available) Less << - -
NCT00002874 - Active, not recruiting - -
NCT00657904 Non-metastatic Prostate Cancer Phase 3 Completed - -
NCT01039233 Bioequivalency Phase 1 Completed - Canada, Quebec ... More >> SFBC Anapharm Montreal, Quebec, Canada, H3X 2H9 Less <<
NCT00871585 - Completed - Croatia ... More >> Research Site Cakovec, Croatia Research Site Dubrovnik, Croatia Research Site Karlovac, Croatia Research Site Pula, Croatia Research Site Rijeka, Croatia Research Site Sibenik, Croatia Research Site Sisak, Croatia Research Site Slavonski brod, Croatia Research Site Split, Croatia Research Site Vinkovci, Croatia Research Site Virovitica, Croatia Research Site Vukovar, Croatia Research Site Zabok, Croatia Research Site Zadar, Croatia Research Site Zagreb, Croatia Less <<
NCT00468715 Breast Cancer Phase 2 Active, not recruiting March 2019 United States, California ... More >> UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, District of Columbia Lombardi Comprehensive Cancer Center at Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Massachusetts Dana-Farber/Harvard Cancer Center at Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 United States, New York Ralph Lauren Center for Cancer Care and Prevention New York, New York, United States, 10035 Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 United States, North Carolina Lineberger Comprehensive Cancer Center at University of North Carolina - Chapel Hill Chapel Hill, North Carolina, United States, 27599-7295 Duke Cancer Institute Durham, North Carolina, United States, 27710 Less <<
NCT00094328 Puberty, Precocious Phase 2 Completed - United States, Alabama ... More >> Research Site Birmingham, Alabama, United States, 35233 United States, Florida Research Site Jacksonville, Florida, United States, 32207 United States, Indiana Research Site Indianapolis, Indiana, United States, 46202 United States, Minnesota Research Site Minneapolis, Minnesota, United States, 55416 United States, Oklahoma Research Site Tulsa, Oklahoma, United States, 74136 United States, Pennsylvania Research Site Philadelphia, Pennsylvania, United States, 19134 United States, South Carolina Research Site Greenville, South Carolina, United States, 29615 United States, Texas Research Site Temple, Texas, United States, 76508 United States, Washington Research Site Spokane, Washington, United States, 99204 Canada, Ontario Research Site London, Ontario, Canada, N6A 4G5 France Research Site Montpellier Cedex, France, 34295 India Research Site Chennai, India, 600020 Research Site New Dehli, India, 110029 Russian Federation Research Site Moscow, Russian Federation, 117036 United Kingdom Research Site London, United Kingdom, WC1N 3JH Less <<
NCT00757692 Prostate Cancer Phase 2 Completed - Canada, British Columbia ... More >> BC Cancer Agency - Centre for Southern Interior Kelowna, British Columbia, Canada, V1Y 5L3 BC Cancer Agency - Vancouver Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Juravinski Cancer Centre Hamilton, Ontario, Canada, L8V 5C2 Sunnybrook Health Sciences Centre Toronto, Ontario, Canada, M4N 3M5 Less <<
NCT00960310 Prostate Cancer ... More >> Hirsutism Less << Phase 1 Completed - -
NCT03147196 Stage I Prostate Adenocarcinom... More >>a Stage II Prostate Adenocarcinoma Less << Phase 2 Recruiting June 2022 United States, Arizona ... More >> Mayo Clinic in Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Clinical Trials Referral Office    855-776-0015    Mangskau.Toni@mayo.edu    Principal Investigator: Erik P. Castle Less <<
NCT01251861 Recurrent Prostate Carcinoma ... More >> Stage I Prostate Cancer AJCC v7 Stage IIA Prostate Cancer AJCC v7 Stage IIB Prostate Cancer AJCC v7 Stage III Prostate Cancer AJCC v7 Less << Phase 2 Active, not recruiting - -
NCT01416870 Healthy Phase 1 Terminated - -
NCT00094328 - Completed - -
NCT00973050 Healthy Phase 1 Completed - Canada, Quebec ... More >> Anapharm Inc. Sainte-Foy, Quebec, Canada, G1V 2K8 Less <<
NCT01664923 Prostate Cancer Phase 2 Completed - -
NCT01664923 - Completed - -
NCT02614859 Cancer of Prostate Phase 2 Recruiting April 2022 United States, Maryland ... More >> National Cancer Institute Recruiting Bethesda, Maryland, United States, 20892-9760 Contact: Marijo Bilusic, MD       marijo.bilusic@nih.gov    United States, Pennsylvania Fox Chase Cancer Center - Philadelphia Recruiting Philadelphia, Pennsylvania, United States, 19111-2497 Less <<
NCT00972855 Healthy Phase 1 Completed - Canada, Quebec ... More >> Anapharm Inc. Sainte-Foy, Quebec, Canada, G1V 2K8 Less <<
NCT00814788 - Completed - -
NCT00551044 Prostatic Neoplasms COMPLETED 2025-08-05 Wirral University Teaching Hos... More >>pitals NHS Trust, Upton, Wirral, Merseyside, CH48 5PE, United Kingdom Less <<
NCT03650894 Breast Neoplasm Female ... More >> Breast Cancer Breast Carcinoma Breast Tumor Less << Phase 2 Not yet recruiting October 2023 United States, Oregon ... More >> Providence Oncology & Hematology Care Clinic - Eastside Not yet recruiting Portland, Oregon, United States, 97213 Sub-Investigator: Rachel Sanborn, MD          Sub-Investigator: Alison Conlin, MD          Sub-Investigator: Todd Crocenzi, MD          Sub-Investigator: Brendan Curti, MD          Sub-Investigator: John Godwin, MD          Sub-Investigator: Rom Leidner, MD          Sub-Investigator: Rui Li, MD, PhD          Sub-Investigator: Walter Urba, MD, PhD          Principal Investigator: David Page, MD          Sub-Investigator: Herschel Wallen, MD          Sub-Investigator: Moran Amy, PhD Less <<
NCT03090165 Triple Negative Breast Cancer Phase 1 Phase 2 Recruiting September 2019 United States, Illinois ... More >> University of Illinois Cancer Center Recruiting Chicago, Illinois, United States, 60612 Contact: Ayesha Zaidi    312-413-1902    azaidi22@uic.edu    Principal Investigator: Kent Hoskins, MD          United States, Michigan Michigan State University Recruiting Lansing, Michigan, United States, 48910 Contact: Karen Luellen    517-975-9534    karen.luellen@hc.msu.edu    Principal Investigator: Deimante Tamkus, MD          United States, New Jersey Rutgers Cancer Institute of New Jersey Recruiting New Brunswick, New Jersey, United States, 08903 Contact: Alison Haegler    732-235-8060    agh46@cinj.rutgers.edu    Principal Investigator: Nancy Chan, MD          United States, Pennsylvania Penn State Cancer Institute Recruiting Hershey, Pennsylvania, United States, 17033 Contact: Sean Flemings    717-531-5364    sfleming1@pennstatehealth.psu.edu    Principal Investigator: Cristina Truica, MD          United States, Wisconsin University of Wisconsin Recruiting Madison, Wisconsin, United States, 53792 Contact: Cancer Connect    608-262-5223    cancerconnect@uwcarbone.wisc.edu Less <<
NCT01288911 Prostatic Neoplasms Phase 2 Completed - -
NCT00630344 Prostate Cancer Phase 2 Completed - United States, Massachusetts ... More >> Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Less <<
NCT00846976 Prostate Cancer PHASE3 COMPLETED 2025-06-13 Research Site, New York, New Y... More >>ork, United States Less <<
NCT01288911 - Completed - -
NCT02605486 Metastatic Breast Cancer (MBC) Phase 1 Phase 2 Recruiting November 2020 United States, New Jersey ... More >> Memoral Sloan Kettering Cancer Center Recruiting Basking Ridge, New Jersey, United States Contact: Ayca Gucalp, MD    646-888-4536       Memorial Sloan Kettering Monmouth Recruiting Middletown, New Jersey, United States, 07748 Contact: Ayca Gucalp, MD    646-888-4536       United States, New York Memorial Sloan Kettering Cancer Center @ Suffolk Recruiting Commack, New York, United States, 11725 Contact: Ayca Gucalp, MD    646-888-4536       Memorial Sloan Kettering Westchester Recruiting Harrison, New York, United States, 10604 Contact: Ayca Gucalp, MD    646-888-4536       Memorial Sloan Kettering at Mercy Medical Center Recruiting Rockville Centre, New York, United States Contact: Ayca Gucalp, MD    646-888-4536 Less <<
NCT01809691 Prostate Cancer Phase 3 Active, not recruiting October 2027 -
NCT00866554 Prostate Cancer ... More >> Erectile Dysfunction Lower Urinary Tract Symptoms Less << Phase 2 Unknown December 2015 Canada ... More >> CHUQ- Hotel-Dieu de Quebec Quebec, Canada, G1R 2J6 Less <<
NCT01044706 Healthy PHASE1 COMPLETED 2025-07-05 SFBC Anapharm, sainte-Foy, Que... More >>bec, G1V 2K8, Canada Less <<
NCT00814788 Prostate Cancer Phase 2 Completed - United States, California ... More >> University of California Davis Cancer Center Sacramento, California, United States, 95817 Less <<
NCT02910050 Breast Cancer Phase 2 Recruiting December 2018 China, Guangdong ... More >> State Key Laboratory of Oncology in South China,Sun Yat-sen University Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Fei Xu, MD    +86-13711277870    xufei@sysucc.org.cn Less <<
NCT01044706 Healthy PHASE1 COMPLETED 2025-07-05 SFBC Anapharm, sainte-Foy, Que... More >>bec, G1V 2K8, Canada Less <<
NCT02348281 Breast Cancer PHASE2 TERMINATED 2025-12-15 Fudan University Shanghai Canc... More >>er Center, Shanghai, 200032, China Less <<
NCT02353988 Breast Neoplasms Phase 2 Unknown May 2017 -
NCT02146937 Detectable Prostate Nodules Phase 2 Withdrawn(Due to lack of accru... More >>al for this study. PI decided to close the study.) Less << - United States, Maryland ... More >> Johns Hopkins Hospital Baltimore, Maryland, United States, 21205 Less <<
NCT02697032 Breast Cancer Phase 2 Recruiting April 2019 Netherlands ... More >> University Medical Center Groningen Recruiting Groningen, Netherlands, 9713 GZ Contact: C. P. Schröder, MD, PhD    +3150 3612821    c.p.schroder@umcg.nl    Contact: G. A.P. Hospers, MD, PhD    +31 50 3612821    g.a.p.hospers@umcg.nl    Principal Investigator: C. P. Schröder, MD, PhD Less <<
NCT03055312 Metastatic Triple Negative Bre... More >>ast Cancer Less << Phase 3 Recruiting December 2020 China, Guangdong ... More >> Sun Yat-sen University Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Zhong-yu Yuan, MD    86-20-87342496    yuanzhy@sysucc.org.cn    Contact: Yong-yi Zhong, BD    86-20-87342635    zhongyy@sysucc.org.cn    Sun Yat-sen University, Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Yuan Zhong-yu, MD    86-20-87342496    yuanzhy@sysucc.org.cn    Contact: Huang Jia-Jia, MD    86-20-87343794    huangjiaj@sysucc.org.cn    Principal Investigator: Yuan Zhong-yu, MD          Sub-Investigator: Huang Jia-Jia, MD Less <<
NCT00630344 - Completed - -
NCT02487823 Non Castrate Metastatic Prosta... More >>te Cancer Less << Phase 1 Terminated(Defect of recruitme... More >>nt) Less << - France ... More >> Institut Paoli Calmettes Marseille, France, 13009 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.62mL

2.32mL

1.16mL

23.24mL

4.65mL

2.32mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]The Protective Role Of Ascorbic Acid Administration On The Bicalutamide Induced Reduction In Semen Quality In The Sprague - Dawley Rat

[2]Cockshott ID, Plummer GF, et al. The pharmacokinetics of Casodex in laboratory animals. Xenobiotica. 1991 Oct;21(10):1347-55.

[3]Attar RM, Jure-Kunkel M, et al. Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer. Cancer Res. 2009 Aug 15;69(16):6522-30.

[4]Sirotnak FM, She Y, et al. Studies with CWR22 xenografts in nude mice suggest that ZD1839 may have a role in the treatment of both androgen-dependent and androgen-independent human prostate cancer. Clin Cancer Res. 2002 Dec;8(12):3870-6.

[5]Shukla GC, Plaga AR, Shankar E, Gupta S. Androgen receptor-related diseases: what do we know? Andrology. 2016 May;4(3):366-81. doi: 10.1111/andr.12167. Epub 2016 Mar 16. PMID: 26991422.

[6]Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20. PMID: 22266222; PMCID: PMC3306502.

[7]Squillace RM, Miller D, Wardwell SD, Wang F, Clackson T, Rivera VM. Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models. Int J Oncol. 2012 Aug;41(2):425-32. doi: 10.3892/ijo.2012.1487. Epub 2012 May 18. PMID: 22614157; PMCID: PMC3582879.

 

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