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Enzalutamide (Synonyms: MDV3100)

Cat. No.: HY-70002 Purity: 99.18%
Data Sheet SDS Handling Instructions

Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

For research use only. We do not sell to patients.
Enzalutamide Chemical Structure

Enzalutamide Chemical Structure

CAS No. : 915087-33-1

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Other Forms of Enzalutamide:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

IC50 & Target

IC50: 36 nM (androgen-receptor, in LNCaP cells)[1]

In Vitro

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide inhibits the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys)[1]. Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex[2].

In Vivo

Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg[1]. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01902251 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Prostate Cancer|Pharmacokinetics of Enzalutamide November 2012 Phase 1
NCT01927627 Case Comprehensive Cancer Center Adenocarcinoma of the Prostate November 11, 2013 Phase 2
NCT02124668 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Castration-Resistant Prostate Cancer|Prostate Cancer September 30, 2014 Phase 2
NCT03207529 M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development, Inc. Malignant Neoplasm of Breast August 2017 Phase 1
NCT02138162 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Severe Hepatic Impairment|Normal Hepatic Function August 2013 Phase 1
NCT01942837 Dana-Farber Cancer Institute|Medivation, Inc. Prostate Cancer September 2013 Phase 2
NCT02953860 University of Colorado, Denver|United States Department of Defense Breast Cancer July 2017 Phase 2
NCT03196388 Fundación Canaria de Investigación Sanitaria|Hospital Universitario de Canarias Prostate Carcinoma June 2017 Phase 2
NCT02500901 Paul Mathew, MD|Hoosier Cancer Research Network|Tesaro, Inc. Metastatic Prostate Cancer March 2016 Phase 1
NCT02138799 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Drug-Drug Interaction (DDI)|Healthy Subjects|Pharmacokinetics of Enzalutamide July 2013 Phase 1
NCT02605863 University of Rochester|Astellas Pharma Inc Bladder Cancer January 2016 Phase 2
NCT02922218 Centro Nacional de Investigaciones Oncologicas CARLOS III|Fundación Pública Andaluza para la Investigación de Málaga en Biomedicina y Salud Prostate Cancer|Castration Resistant|Enzalutamide June 2016
NCT03124615 Macquarie University, Australia Prostate Cancer May 2017 Phase 2
NCT02028988 Dana-Farber Cancer Institute|Medivation, Inc. Intermediate Risk Prostate Cancer January 2014 Phase 2
NCT02684227 M.D. Anderson Cancer Center|Astellas Pharma Inc|Medivation, Inc.|National Comprehensive Cancer Network Endometrial Cancer August 2016 Phase 2
NCT02384382 Medivation, Inc.|Astellas Pharma Inc|Pfizer Prostate Carcinoma Metastatic to the Bone|Castration Resistant Prostate Cancer November 2015 Phase 2
NCT02116582 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration-Resistant Prostate Cancer April 11, 2014 Phase 4
NCT02288936 Spanish Oncology Genito-Urinary Group Hormone-refractory Prostate Cancer February 5, 2015 Phase 2
NCT02207504 Dana-Farber Cancer Institute|Astellas Pharma Inc|Pfizer Castration-resistant Prostate Cancer August 2014 Phase 1
NCT02441517 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration Resistant Prostate Cancer October 28, 2015 Phase 4
NCT01302041 Astellas Pharma Inc|Medivation, Inc. Prostate Cancer May 6, 2011 Phase 2
NCT01664923 Medivation, Inc.|Astellas Pharma Inc Prostate Cancer August 2012 Phase 2
NCT01977651 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration-resistant Prostate Cancer (mCRPC) September 24, 2013 Phase 4
NCT02003924 Pfizer|Astellas Pharma Inc|Medivation, Inc. Nonmetastatic Castration-Resistant Prostate Cancer|Prostate Cancer|Cancer of the Prostate December 2013 Phase 3
NCT02203695 Sidney Kimmel Comprehensive Cancer Center|Astellas Pharma Inc|Medivation, Inc. Adenocarcinoma of the Prostate August 2014 Phase 2
NCT01974765 Memorial Sloan Kettering Cancer Center|Medivation, Inc. Advanced Epithelial Ovarian|Recurrent Epithelial Ovarian|Fallopian Tube|Primary Peritoneal Carcinoma November 2013 Phase 2
NCT02125084 SCRI Development Innovations, LLC|Novartis Pharmaceuticals Prostate Cancer October 2014 Phase 1
NCT03123978 University of California, Davis|National Cancer Institute (NCI)|Pandomedx Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer June 2017 Phase 1
NCT02064582 University of Texas Southwestern Medical Center|Astellas Pharma US, Inc. Prostate Cancer May 2014 Phase 2
NCT02495974 Astellas Pharma Europe Ltd.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration Resistant Prostate Cancer September 8, 2015
NCT02929576 Medivation, Inc.|Astellas Pharma Inc Breast Cancer September 2016 Phase 3
NCT02960022 Astellas Pharma Global Development, Inc.|Medivation, Inc., a wholly owned subsidiary of Pfizer Inc.|Astellas Pharma Inc Prostate Cancer December 22, 2016 Phase 2
NCT02294461 Astellas Pharma Inc Progressive Metastatic Prostate Cancer April 23, 2014 Phase 3
NCT01663415 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration-Resistant Prostate Cancer August 2012 Phase 2
NCT01889238 Medivation, Inc.|Astellas Pharma Inc Advanced, Androgen Receptor Positive Triple Negative Breast Cancer June 2013 Phase 2
NCT02711956 Zenith Epigenetics Metastatic Castration-Resistant Prostate Cancer December 2016 Phase 1
NCT02528643 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Advanced Hepatocellular Carcinoma November 9, 2015 Phase 2
NCT02750358 Memorial Sloan Kettering Cancer Center|Medivation, Inc.|Astellas Pharma Inc Breast Cancer|Early Stage|Triple Negative Breast Cancer May 19, 2016 Phase 2
NCT02007512 Medivation, Inc.|Astellas Pharma Inc Breast Cancer December 2013 Phase 2
NCT02319837 Medivation, Inc.|Astellas Pharma Inc Hormone Sensitive Prostate Cancer|Prostate Cancer|Cancer of the Prostate December 2014 Phase 3
NCT02918968 Astellas Pharma Inc|Medivation, Inc. Prostate Cancer November 2, 2016 Phase 4
NCT03177187 Institute of Cancer Research, United Kingdom|Astellas Pharma Inc|AstraZeneca|Prostate Cancer UK Metastatic Castration Resistant Prostate Cancer June 2017 Phase 1|Phase 2
NCT03016312 Hoffmann-La Roche Prostatic Neoplasms, Castration-Resistant January 11, 2017 Phase 3
NCT02677896 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Hormone Sensitive Prostate Cancer March 7, 2016 Phase 3
NCT02057939 Duke University|Medivation, Inc.|Astellas Pharma Inc Prostate Cancer April 2014 Phase 2
NCT02452008 Sidney Kimmel Comprehensive Cancer Center Prostate Cancer April 2016 Phase 2
NCT02642913 Memorial Sloan Kettering Cancer Center|Astellas Pharma US, Inc.|Mayo Clinic|University of California, San Francisco|University of Southern California|Washington University School of Medicine|Roswell Park Cancer Institute|National Comprehensive Cancer Network|Mayo Clinic Florida Hepatocellular Carcinoma December 2015 Phase 1|Phase 2
NCT02099864 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Hormone-Resistant Prostate Cancer|Metastatic Prostatic Adenocarcinoma|Recurrent Prostate Carcinoma|Stage III Prostate Adenocarcinoma|Stage IV Prostate Adenocarcinoma February 2014
NCT02339168 University of California, Davis|National Cancer Institute (NCI)|Medivation, Inc.|Astellas Pharma Inc Prostate Cancer June 2016 Phase 1
NCT02489123 University of Washington|National Cancer Institute (NCI)|National Comprehensive Cancer Network Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma|Stage I Mantle Cell Lymphoma|Stage II Mantle Cell Lymphoma|Stage III Mantle Cell Lymphoma|Stage IV Mantle Cell Lymphoma August 11, 2015
NCT02689427 M.D. Anderson Cancer Center|Astellas Pharma US, Inc. Breast Cancer September 2016 Phase 2
NCT02955394 University of Colorado, Denver|United States Department of Defense Breast Cancer July 2017 Phase 2
NCT02555189 Sidney Kimmel Cancer Center at Thomas Jefferson University|Novartis|Prostate Cancer Clinical Trials Consortium|Thomas Jefferson University Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Carcinoma Metastatic in the Bone|Stage IV Prostate Cancer December 2015 Phase 1|Phase 2
NCT02640534 Swiss Group for Clinical Cancer Research Cancer of the Prostate|Prostate Cancer March 24, 2016 Phase 2
NCT01995513 Medivation, Inc.|Astellas Pharma Inc Prostate Cancer November 2013 Phase 4
NCT02012296 University of Chicago|National Cancer Institute (NCI) Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer December 2013 Phase 1|Phase 2
NCT01547299 Medivation, Inc.|Astellas Pharma Inc Prostate Cancer March 2012 Phase 2
NCT01597193 Medivation, Inc.|Astellas Pharma Inc Breast Cancer April 2012 Phase 1
NCT01650194 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration-Resistant Prostate Cancer July 9, 2012 Phase 2
NCT02429193 University Health Network, Toronto Castration-resistant Prostate Cancer March 2016 Phase 2
NCT02935205 University of California, Davis|National Cancer Institute (NCI) Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer January 2017 Phase 1|Phase 2
NCT02749903 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Astellas Pharma US, Inc. Salivary Cancer June 2016 Phase 2
NCT02833883 Memorial Sloan Kettering Cancer Center|Celgene Corporation Prostate Cancer|Castration Resistant Prostate Cancer July 2016 Phase 1
NCT02607228 Gilead Sciences Metastatic Castrate-Resistant Prostate Cancer December 8, 2015 Phase 1|Phase 2
NCT02799745 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Prostate Cancer May 24, 2016 Phase 2
NCT02885649 Rutgers, The State University of New Jersey|National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Stage I Renal Cell Cancer October 2017 Early Phase 1
NCT01981122 Dendreon Metastatic Prostate Cancer September 2013 Phase 2
NCT02228265 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Prostate Adenocarcinoma|PSA Progression|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer March 12, 2013
NCT02213107 University of Rochester Prostate Cancer September 2014 Phase 2
NCT02457910 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Translational Breast Cancer Research Consortium|Conquer Cancer Foundation|Genentech, Inc. Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Progesterone Receptor Negative|Progesterone Receptor Positive|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma June 2015 Phase 1|Phase 2
NCT02588001 Translational Research Informatics Center, Kobe, Hyogo, Japan|Kagawa University Prostate Cancer October 2015
NCT01288911 Astellas Pharma Inc|Medivation, Inc. Prostatic Neoplasms March 2, 2011 Phase 2
NCT00974311 Medivation, Inc.|Astellas Pharma Inc Castration-Resistant Prostate Cancer September 2009 Phase 3
NCT02091960 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc HER2 Amplified|Advanced Breast Cancer|Human Epidermal Growth Factor Receptor 2 (HER2) August 28, 2014 Phase 2
NCT02353715 Duke University Prostate Cancer May 2015
NCT02438007 Tokai Pharmaceuticals Prostate Cancer June 2015 Phase 3
NCT02215096 GlaxoSmithKline Cancer November 13, 2014 Phase 1
NCT02225704 Cancer Trials Ireland Prostate Cancer June 2015 Phase 2
NCT02125357 British Columbia Cancer Agency Metastatic Castration-Resistant Prostate Cancer September 2014 Phase 2
NCT02532114 University of Washington|National Cancer Institute (NCI) Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Adenocarcinoma December 2015 Phase 1
NCT02199197 University of Utah Prostate Cancer June 2014 Phase 2
NCT02288247 Astellas Pharma Europe Ltd.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration Resistant Prostate Cancer December 1, 2014 Phase 3
NCT02507570 Carolina Research Professionals, LLC|Astellas Pharma Inc Prostate Carcinoma Metastatic to the Bone September 2015 Phase 2
NCT01885949 Massachusetts General Hospital|National Comprehensive Cancer Network Prostate Cancer June 2013 Phase 2
NCT01949337 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Astellas Pharma US, Inc.|Medivation, Inc.|Biologics, Inc. Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer January 2014 Phase 3
NCT01091103 Medivation, Inc.|Astellas Pharma Inc Metastatic Progressive Castration-resistant Prostate Cancer February 2010 Phase 2
NCT02286921 Sidney Kimmel Comprehensive Cancer Center|United States Department of Defense Castration Resistant Metastatic Prostate Cancer January 2015 Phase 2
NCT02300610 H. Lee Moffitt Cancer Center and Research Institute Bladder Cancer|Carcinoma, Transitional Cell|Renal Pelvis Cancer|Ureter Cancer|Urethra Cancer February 11, 2015 Phase 1
NCT02491411 Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Adenocarcinoma|Stage IV Prostate Cancer September 2015
NCT02407054 Eli Lilly and Company|Sarah Cannon Development Innovations Prostate Cancer Metastatic April 2015 Phase 2
NCT02525068 Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust Adenocarcinoma of the Prostate December 2014 Phase 2
NCT02508636 University of California, San Francisco|National Comprehensive Cancer Network Prostatic Neoplasms|Pelvic Nodal August 2015 Phase 2
NCT02023463 Sidney Kimmel Cancer Center at Thomas Jefferson University|Astellas Pharma Inc|Medivation, Inc.|Thomas Jefferson University Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer April 2014 Phase 1
NCT02138383 H. Lee Moffitt Cancer Center and Research Institute|Astellas Pharma Inc Pancreatic Cancer May 22, 2014 Phase 1
NCT02446405 University of Sydney|Australian and New Zealand Urogenital and Prostate Cancer Trials Group|National Health and Medical Research Council, Australia|Cancer Trials Ireland|NCIC Clinical Trials Group Prostatic Neoplasms March 2014 Phase 3
NCT01946165 M.D. Anderson Cancer Center|Janssen Services, LLC|Medivation, Inc. Prostate Cancer October 2013 Phase 2
NCT02453009 Santa Chiara Hospital Prostatic Neoplasms October 2014 Phase 2
NCT02254785 British Columbia Cancer Agency|Sanofi|Ozmosis Research Inc. Metastatic Castration-Resistant Prostatic Cancer October 2014 Phase 2
NCT02346578 Taro Iguchi, MD, PHD|Astellas Pharma Inc|Osaka City University Castration-resistant Prostate Cancer January 2015
NCT02987543 AstraZeneca Metastatic Castration-resistant Prostate Cancer February 6, 2017 Phase 3
NCT02522715 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer June 28, 2015 Phase 1|Phase 2
NCT02312557 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Castration-Resistant Prostate Carcinoma|Hormone-Resistant Prostate Cancer|PSA Progression|Recurrent Prostate Carcinoma|Stage IV Prostate Adenocarcinoma November 18, 2014 Phase 2
NCT02225093 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Pharmacokinetics of Dextromethorphan|Pharmacokinetics of Caffeine|Prostate Cancer October 2, 2013 Phase 1
NCT02471469 Radboud University|Astellas Pharma Europe B.V. Metastatic Castration Resistant Prostate Cancer October 2015
NCT02090114 Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) Prostate Cancer June 2014 Phase 2
NCT02204072 Boehringer Ingelheim Prostatic Neoplasms, Castration-Resistant November 11, 2014 Phase 1
NCT02380313 GlaxoSmithKline Cancer October 2015 Phase 1
NCT01212991 Medivation, Inc.|Astellas Pharma Inc Prostate Cancer September 2010 Phase 3
NCT02685267 Prostate Cancer Clinical Trials Consortium|University of Chicago|Astellas Pharma Inc Prostate Cancer February 2016 Phase 2
NCT02676986 Queen Mary University of London|Astellas Pharma Inc Primary Breast Cancer ER+ve|Primary Breast Cancer AR+ve TNBN August 2015 Phase 2
NCT02485691 Sanofi Prostate Cancer Metastatic November 2015 Phase 4
NCT02268175 Dana-Farber Cancer Institute|Medivation, Inc. Prostate Adenocarcinoma|Prostate Cancer|High Risk Prostate Cancer October 2014 Phase 2
NCT02446444 University of Sydney|Australian and New Zealand Urogenital and Prostate Cancer Trials Group|National Health and Medical Research Council, Australia|Cancer Trials Ireland|TROG- Trans Tasman Radiation Oncology Group Prostatic Neoplasms March 2014 Phase 3
NCT02278185 University of Colorado, Denver Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer November 11, 2015 Phase 2
NCT02058706 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage IV Prostate Cancer May 2014 Phase 2
NCT01875250 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Prostate Cancer May 28, 2013 Phase 2
NCT02815033 The European Uro-Oncology Group|Centre for Human Drug Research, Netherlands Prostate Cancer Metastatic July 2015 Phase 2
NCT02814968 The European Uro-Oncology Group|Centre for Human Drug Research, Netherlands Prostate Cancer Metastatic February 2015 Phase 2
NCT02194842 European Organisation for Research and Treatment of Cancer - EORTC|Bayer|Astellas Pharma Europe Ltd.|Academic and Community Cancer Research United|Cancer Trials Ireland|UNICANCER|GETUG Prostate Cancer October 2015 Phase 3
NCT02034552 Bayer Prostatic Neoplasms December 30, 2013 Phase 2
NCT01867333 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Prostate Cancer May 16, 2013 Phase 2
NCT01362374 Genentech, Inc. Neoplasms July 11, 2011 Phase 1
NCT02256111 Duke University Non-metastatic, Hormone naïve Prostate Cancer May 13, 2015 Phase 2
NCT02159690 Kenneth Pienta, MD|Prostate Cancer Foundation Norway|Johns Hopkins University Prostate Cancer|Localized Prostate Cancer September 2014 Phase 2
NCT02758132 University of Hawaii Prostate Cancer July 2015
NCT02975934 Clovis Oncology, Inc.|Foundation Medicine Metastatic Castration Resistant Prostate Cancer January 2017 Phase 3
NCT02991911 MedImmune LLC Metastatic Castration Resistant Prostate Cancer January 6, 2017 Phase 1
NCT03150056 GlaxoSmithKline Solid Tumours May 31, 2017 Phase 1
NCT03016741 Vanderbilt-Ingram Cancer Center Castration-Resistant Prostatic Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer|Hormone-Refractory Prostate Cancer March 31, 2017 Phase 4
NCT02685397 Sir Mortimer B. Davis - Jewish General Hospital Castration-resistant Prostate Cancer Patients With Oligometastases August 2016 Phase 2|Phase 3
NCT00268476 Medical Research Council Prostate Cancer September 2005 Phase 2|Phase 3
NCT02787005 Merck Sharp & Dohme Corp. Metastatic Castration-resistant Prostate Cancer July 1, 2016 Phase 2
NCT02861573 Merck Sharp & Dohme Corp. Metastatic Castration-Resistant Prostate Cancer November 17, 2016 Phase 1
NCT01990196 Jonsson Comprehensive Cancer Center Prostate Cancer September 23, 2014 Phase 2
NCT02580448 Innocrin Pharmaceutical Cancer of the Breast|Breast Cancer|Advanced Breast Cancer|Metastatic Breast Cancer|Male Breast Cancer|Triple Negative Breast Cancer|ER+ Breast Cancer August 2015 Phase 1|Phase 2
NCT02903160 Icahn School of Medicine at Mount Sinai|Sanofi|Bayer Prostate Cancer October 2016 Phase 2
NCT01565928 Medivation, Inc.|Astellas Pharma Inc Prostate Cancer February 2012 Phase 1
NCT01911728 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Pharmacokinetics of MDV3100|Castration Resistant Prostate Cancer (CRPC) July 25, 2011 Phase 1
NCT01911715 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of MDV3100 April 2011 Phase 1
NCT01901133 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Pharmacokinetics of MDV3100|Healthy Subjects|Kidney Diseases October 2011 Phase 1
NCT01534052 Astellas Pharma Inc|Medivation, Inc. Castration-Resistant Prostate Cancer (CRPC) October 26, 2011 Phase 2
NCT01911741 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Healthy Subjects|Castration Resistant Prostate Cancer (CRPC)|Relative Bioavailability|MDV3100 November 2012 Phase 1
NCT00510718 Medivation, Inc. Prostate Cancer|Hormone Refractory Prostate Cancer July 2007 Phase 1
NCT01913379 Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics|Drug-Drug Interaction August 2011 Phase 1
NCT01606982 Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc Metastatic Castration-Resistant Prostate Cancer
NCT01284920 Astellas Pharma Inc Prostate Neoplasms|Prostate Cancer|Castration Resistant Prostate Cancer (CRPC) November 2010 Phase 1|Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.1531 mL 10.7657 mL 21.5313 mL
5 mM 0.4306 mL 2.1531 mL 4.3063 mL
10 mM 0.2153 mL 1.0766 mL 2.1531 mL
Cell Assay
[1]

Enzalutamide is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1].

LNCaP cells (107 cells/condition) are grown in RPMI media supplemented with 5% charcoalstripped serum for 22 days, then treated with DMSO or 1 nM R1881, combined with an antiandrogen (DMSO, 1 μM Bicalutamide, 10 μM Bicalutamide, 1 μM RD162, 10 μM RD162, 1 μM MDV3100, or 10 μM MDV3100) for 8 hours. An aliquot of cells are harvested for qRT-PCR of PSA and TMPRSS2 mRNA. The remaining cells are cross-linked using 1% paraformaldehyde for 10 minutes, then glycine is added and samples centrifuged (4°C, 4000 rpm, 5 minutes) to stop further crosslinking. Chromatin immunoprecipitation is performed using a chromatin immunoprecipitation assay kit. Immunoprecipitated DNA is amplified by real-time PCR. Primers are PSA enhancer forward-ATGTTCACATTAGTACACCTTGCC and reverse-TCTCAGATCCAGGCTTGCTTACTGTC and TMPRSS2 enhancer forward-TGGTCCTGGATGATAAAAAAAGTTT and reverse-GACATACGCCCCACAACAGA[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Enzalutamide is dissolved in vehicle (10 % DMSO, 45 % polyethylene glycol 400, and 45 % saline) (Rat)[4].

Mice[3]
Following a 5-day acclimation period, 5- to 9-week-old male CB17SCID mice are castrated and allowed to recover for an additional 5 days before inoculation with tumor cells. LNCaP cells co-expressing exogenous AR and the AR-dependent reporter construct ARR2-Pb-Luc (LNCaP-AR-Lux cells) are used to generate a xenograft model of human prostate cancer. Before implantation, LNCaP-AR-Lux cells are prepared by the addition of trypsin-EDTA, washed with complete medium, collected and resuspended at 20×106 cells/mL. Cell suspensions are diluted with Matrigel to 2×106 cells/0.2 mL and delivered subcutaneously in the suprascapular region. Tumor growth is monitored to the volume of 100 mm3 when treatment begins (80 days). The observed rate of tumor take with LNCaP-AR-Lux cells is between 70% and 80%. Body weight and tumor volumes (width2×length/2) are measured two to three times per week with a digital caliper, and the average tumor volumes are determined. Test drugs are diluted in Tween 80:PEG 400, and stored at 4°C until administration by oral gavage. Each group of mice (n=7) is treated daily for 28 consecutive days with 1, 10, or 50 mg/kg Enzalutamide, vehicle control, or 50 mg/kg Bicalutamide. At the end of the treatment period or when tumor volume exceeded 1,000 mm3, animals are euthanized and blood and tissue samples are collected for analysis.
Rat[4]
Male SD rats (n=3) are administered Enzalutamide through the tail vein (intravenous) and by oral gavage at 1 mg/kg and are kept in metabolic cages after dosing. Urine and feces samples are collected over the following time intervals after dosing: 0-2, 2-4, 4-6, 6-10, 10-24, 24-48, and 48-72 h. The metabolic cages are rinsed with distilled water, and residues are added to the urine samples at 72 h. To extract the Enzalutamide present in the feces, samples are shaken vigorously for 12 h with 50 % methanol. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

464.44

Formula

C₂₁H₁₆F₄N₄O₂S

CAS No.

915087-33-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.18%

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Product Name:
Enzalutamide
Cat. No.:
HY-70002
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