1. Protein Tyrosine Kinase/RTK
  2. PDGFR
    VEGFR
    FGFR

BIBF 1120 (Synonyms: Nintedanib)

Cat. No.: HY-50904 Purity: 99.72%
Data Sheet SDS Handling Instructions

BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

For research use only. We do not sell to patients.
BIBF 1120 Chemical Structure

BIBF 1120 Chemical Structure

CAS No. : 656247-17-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $61 In-stock
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500 mg $340 In-stock
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Customer Review

Other Forms of BIBF 1120:

    BIBF 1120 purchased from MCE. Usage Cited in: Oncol Rep. 2016 Dec;36(6):3123-3130.

    The concentration of Trifluridine incorporated in the DNA in the human colorectal HT-29 (A) and HCT116 (B) xenografts. The mice are treated with TFTD alone (150 mg/kg, orally twice daily from days 1 to 14, open column), or a combination of TFTD and Nintedanib (closed column). The HT-29 and HCT116 tumors are collected at 24 h following the final administration of the drugs (day 15). The values indicate the mean ± SD (n=6).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

    IC50 & Target

    IC50: 34 nM (VEGFR1), 13 nM (VEGFR2), 13 nM (VEGFR3), 69 nM (FGFR1), 37 nM (FGFR1), 108 nM (FGFR1), 59 nM (PDGFRα), 65 nM (PDGFRβ)

    In Vitro

    BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)[1].

    In Vivo

    BIBF1120 (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition[1]. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01349296 University of Cologne|Boehringer Ingelheim Solid Tumors July 2012 Phase 1
    NCT01669798 AA Secord|Boehringer Ingelheim|Duke University Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer February 2013 Phase 2
    NCT01619085 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis June 2012 Phase 3
    NCT01610869 University College, London|Boehringer Ingelheim Ovarian Cancer|Fallopian Tube Cancer August 2014 Phase 2
    NCT02182076 Boehringer Ingelheim Healthy October 2005 Phase 1
    NCT02182128 Boehringer Ingelheim Tumors June 2006 Phase 1
    NCT01951846 Boehringer Ingelheim Malignant Solid Tumour November 2002 Phase 1
    NCT02182206 Boehringer Ingelheim Tumors June 2003 Phase 1
    NCT01346540 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 14, 2011 Phase 1
    NCT01684111 Aktion Bronchialkarzinom e.V.|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung June 2013 Phase 1
    NCT01022853 Boehringer Ingelheim Neoplasms December 2009 Phase 1
    NCT01485874 Hoosier Cancer Research Network|Boehringer Ingelheim Ovarian Cancer November 2011 Phase 1
    NCT02182219 Boehringer Ingelheim Prostatic Neoplasms November 2005 Phase 1
    NCT01024920 Boehringer Ingelheim Carcinoma, Renal Cell December 2009 Phase 2
    NCT00998296 Boehringer Ingelheim Neoplasms October 2009 Phase 1
    NCT02182102 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung September 2005 Phase 1
    NCT02389764 M.D. Anderson Cancer Center|Boehringer Ingelheim Breast Cancer June 2015 Phase 2
    NCT01666600 Prof. Dr. Wolfgang Wick|University Hospital Heidelberg Glioblastoma Multiforme August 2012 Phase 1|Phase 2
    NCT01335477 Boehringer Ingelheim Pulmonary Fibrosis May 2011 Phase 3
    NCT00805194 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 3, 2008 Phase 3
    NCT01329549 Boehringer Ingelheim Ovarian Neoplasms April 2011 Phase 1
    NCT01314105 Boehringer Ingelheim Ovarian Neoplasms|Peritoneal Neoplasms March 2011 Phase 1
    NCT01335464 Boehringer Ingelheim Pulmonary Fibrosis April 2011 Phase 3
    NCT01683682 Aktion Bronchialkarzinom e.V.|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2013 Phase 1
    NCT00876460 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2009 Phase 1
    NCT02182141 Boehringer Ingelheim Multiple Myeloma April 2003 Phase 1
    NCT01441297 Ji-youn Han|National Cancer Center, Korea Small Cell Lung Cancer|Small Cell Lung Cancer Recurrent December 2011 Phase 2
    NCT02182232 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung June 2005 Phase 1
    NCT00730821 Boehringer Ingelheim Neoplasms January 2007 Phase 1
    NCT01170065 Boehringer Ingelheim Pulmonary Fibrosis June 2010 Phase 2
    NCT02182063 Boehringer Ingelheim Prostatic Neoplasms November 2005 Phase 2
    NCT01380782 Patrick Y. Wen, MD|Boehringer Ingelheim|Wake Forest University Health Sciences|University of Virginia|Massachusetts General Hospital|The Cleveland Clinic|Dana-Farber Cancer Institute Glioblastoma|Gliosarcoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Anaplastic Oligoastrocytoma May 2012 Phase 2
    NCT02182245 Boehringer Ingelheim Genital Neoplasms, Female October 2005 Phase 1
    NCT00979576 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 1
    NCT00904839 Boehringer Ingelheim Colorectal Neoplasms May 2009 Phase 2
    NCT00715403 Boehringer Ingelheim Neoplasms October 2004 Phase 1
    NCT01004003 Boehringer Ingelheim Carcinoma, Hepatocellular October 2009 Phase 2
    NCT02182154 Boehringer Ingelheim Healthy October 2005 Phase 1
    NCT01136174 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis May 2010 Phase 2
    NCT01015118 Boehringer Ingelheim Ovarian Neoplasms|Peritoneal Neoplasms November 2009 Phase 3
    NCT02182050 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 2005 Phase 2
    NCT00801294 Boehringer Ingelheim Colorectal Neoplasms July 2006 Phase 2
    NCT02182193 Boehringer Ingelheim Healthy September 2006 Phase 1
    NCT02182258 Boehringer Ingelheim Healthy June 2009 Phase 1
    NCT01362361 Martin-Luther-Universität Halle-Wittenberg|GALMED GmbH, Halle, Germany Colorectal Cancer June 2011 Phase 2
    NCT00987935 Boehringer Ingelheim Carcinoma, Hepatocellular October 2009 Phase 2
    NCT00706628 Boehringer Ingelheim Prostatic Neoplasms March 2006 Phase 2
    NCT00514683 Boehringer Ingelheim Pulmonary Fibrosis August 2007 Phase 2
    NCT02149108 Boehringer Ingelheim Colorectal Neoplasms September 25, 2014 Phase 3
    NCT02152059 AHS Cancer Control Alberta|Cross Cancer Institute|Boehringer Ingelheim Small Cell Lung Cancer|Platinum-sensitive July 2014 Phase 2
    NCT02278978 National Taiwan University Hospital Urothelial Carcinoma October 2014 Phase 2
    NCT02558387 Samsung Medical Center Recurrent or Metastatic Salivary Gland Cancer of the Head and Neck November 2014 Phase 2
    NCT01488344 University Hospital Muenster|Boehringer Ingelheim Acute Myeloid Leukemia March 2012 Phase 1|Phase 2
    NCT01251484 Ulrik Lassen|Boehringer Ingelheim|University of Copenhagen|Rigshospitalet, Denmark Recurrent Glioblastoma January 2011 Phase 2
    NCT00710762 Boehringer Ingelheim Ovarian Neoplasms March 2006 Phase 2
    NCT00806819 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2008 Phase 3
    NCT01349296 University of Cologne|Boehringer Ingelheim Solid Tumors July 2012 Phase 1
    NCT01669798 AA Secord|Boehringer Ingelheim|Duke University Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer February 2013 Phase 2
    NCT01619085 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis June 2012 Phase 3
    NCT01610869 University College, London|Boehringer Ingelheim Ovarian Cancer|Fallopian Tube Cancer August 2014 Phase 2
    NCT02182076 Boehringer Ingelheim Healthy October 2005 Phase 1
    NCT02182128 Boehringer Ingelheim Tumors June 2006 Phase 1
    NCT01951846 Boehringer Ingelheim Malignant Solid Tumour November 2002 Phase 1
    NCT02182206 Boehringer Ingelheim Tumors June 2003 Phase 1
    NCT01346540 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 14, 2011 Phase 1
    NCT01684111 Aktion Bronchialkarzinom e.V.|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung June 2013 Phase 1
    NCT01022853 Boehringer Ingelheim Neoplasms December 2009 Phase 1
    NCT01485874 Hoosier Cancer Research Network|Boehringer Ingelheim Ovarian Cancer November 2011 Phase 1
    NCT02182219 Boehringer Ingelheim Prostatic Neoplasms November 2005 Phase 1
    NCT01024920 Boehringer Ingelheim Carcinoma, Renal Cell December 2009 Phase 2
    NCT00998296 Boehringer Ingelheim Neoplasms October 2009 Phase 1
    NCT02182102 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung September 2005 Phase 1
    NCT02389764 M.D. Anderson Cancer Center|Boehringer Ingelheim Breast Cancer June 2015 Phase 2
    NCT01666600 Prof. Dr. Wolfgang Wick|University Hospital Heidelberg Glioblastoma Multiforme August 2012 Phase 1|Phase 2
    NCT01335477 Boehringer Ingelheim Pulmonary Fibrosis May 2011 Phase 3
    NCT00805194 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 3, 2008 Phase 3
    NCT01329549 Boehringer Ingelheim Ovarian Neoplasms April 2011 Phase 1
    NCT01314105 Boehringer Ingelheim Ovarian Neoplasms|Peritoneal Neoplasms March 2011 Phase 1
    NCT01335464 Boehringer Ingelheim Pulmonary Fibrosis April 2011 Phase 3
    NCT01683682 Aktion Bronchialkarzinom e.V.|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2013 Phase 1
    NCT00876460 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2009 Phase 1
    NCT02182141 Boehringer Ingelheim Multiple Myeloma April 2003 Phase 1
    NCT01441297 Ji-youn Han|National Cancer Center, Korea Small Cell Lung Cancer|Small Cell Lung Cancer Recurrent December 2011 Phase 2
    NCT02182232 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung June 2005 Phase 1
    NCT00730821 Boehringer Ingelheim Neoplasms January 2007 Phase 1
    NCT01170065 Boehringer Ingelheim Pulmonary Fibrosis June 2010 Phase 2
    NCT02182063 Boehringer Ingelheim Prostatic Neoplasms November 2005 Phase 2
    NCT01380782 Patrick Y. Wen, MD|Boehringer Ingelheim|Wake Forest University Health Sciences|University of Virginia|Massachusetts General Hospital|The Cleveland Clinic|Dana-Farber Cancer Institute Glioblastoma|Gliosarcoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Anaplastic Oligoastrocytoma May 2012 Phase 2
    NCT02182245 Boehringer Ingelheim Genital Neoplasms, Female October 2005 Phase 1
    NCT00979576 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 1
    NCT00904839 Boehringer Ingelheim Colorectal Neoplasms May 2009 Phase 2
    NCT00715403 Boehringer Ingelheim Neoplasms October 2004 Phase 1
    NCT01004003 Boehringer Ingelheim Carcinoma, Hepatocellular October 2009 Phase 2
    NCT02182154 Boehringer Ingelheim Healthy October 2005 Phase 1
    NCT01136174 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis May 2010 Phase 2
    NCT01015118 Boehringer Ingelheim Ovarian Neoplasms|Peritoneal Neoplasms November 2009 Phase 3
    NCT02182050 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 2005 Phase 2
    NCT00801294 Boehringer Ingelheim Colorectal Neoplasms July 2006 Phase 2
    NCT02182193 Boehringer Ingelheim Healthy September 2006 Phase 1
    NCT02182258 Boehringer Ingelheim Healthy June 2009 Phase 1
    NCT01362361 Martin-Luther-Universität Halle-Wittenberg|GALMED GmbH, Halle, Germany Colorectal Cancer June 2011 Phase 2
    NCT00987935 Boehringer Ingelheim Carcinoma, Hepatocellular October 2009 Phase 2
    NCT00706628 Boehringer Ingelheim Prostatic Neoplasms March 2006 Phase 2
    NCT00514683 Boehringer Ingelheim Pulmonary Fibrosis August 2007 Phase 2
    NCT02149108 Boehringer Ingelheim Colorectal Neoplasms September 25, 2014 Phase 3
    NCT02152059 AHS Cancer Control Alberta|Cross Cancer Institute|Boehringer Ingelheim Small Cell Lung Cancer|Platinum-sensitive July 2014 Phase 2
    NCT02278978 National Taiwan University Hospital Urothelial Carcinoma October 2014 Phase 2
    NCT02558387 Samsung Medical Center Recurrent or Metastatic Salivary Gland Cancer of the Head and Neck November 2014 Phase 2
    NCT01488344 University Hospital Muenster|Boehringer Ingelheim Acute Myeloid Leukemia March 2012 Phase 1|Phase 2
    NCT01251484 Ulrik Lassen|Boehringer Ingelheim|University of Copenhagen|Rigshospitalet, Denmark Recurrent Glioblastoma January 2011 Phase 2
    NCT00710762 Boehringer Ingelheim Ovarian Neoplasms March 2006 Phase 2
    NCT00806819 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2008 Phase 3
    NCT02598193 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis January 14, 2016 Phase 4
    NCT02835833 University of Alabama at Birmingham|Boehringer Ingelheim Renal Cell Carcinoma|Colorectal Adenocarcinoma|Non-squamous Non-small Cell Lung Cancer|Platinum-refractory Ovarian Carcinoma|Cervical Carcinoma June 2016 Phase 1
    NCT02902484 University of Texas Southwestern Medical Center|Boehringer Ingelheim|The University of Texas Health Science Center at San Antonio|South Plains Oncology Consortium Cancer of Pancreas January 2017 Phase 1|Phase 2
    NCT01788982 European Organisation for Research and Treatment of Cancer - EORTC Medullary Thyroid Cancer (MTC)|Differentiated Thyroid Cancer (DTC) May 2014 Phase 2
    NCT02234596 Memorial Sloan Kettering Cancer Center Esophagogastric Adenocarcinoma September 2014 Phase 2
    NCT03062943 IRCCS Multimedica Lymphangioleiomyomatosis October 2016 Phase 2
    NCT02299141 Washington University School of Medicine|National Comprehensive Cancer Network Carcinoma, Non-Small-Cell Lung|Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer May 7, 2015 Phase 1
    NCT02579603 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis October 16, 2015 Phase 4
    NCT02225405 M.D. Anderson Cancer Center|Boehringer Ingelheim Lung Cancer April 2015 Phase 1
    NCT02808247 European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim Sarcoma, Soft Tissue July 7, 2017 Phase 2
    NCT02568449 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Recurrent Pleural Malignant Mesothelioma|Stage IV Pleural Mesothelioma October 2015 Phase 2
    NCT02308553 Prof. Dr. med. Dirk Schadendorf|Boehringer Ingelheim|medac GmbH|Alcedis GmbH|University Hospital, Essen Cutaneous Malignant Melanoma January 2015 Phase 1|Phase 2
    NCT02572752 Boehringer Ingelheim Healthy August 2015 Phase 1
    NCT02667704 Boehringer Ingelheim Healthy February 2016 Phase 1
    NCT02619162 Centro Nacional de Investigaciones Oncologicas CARLOS III|Dr. Miguel Angel Quintela Fandiño (CNIO)|Dr, Ramón Colomer i Bosch|FUNDACIÓN CRIS (Marta Cardona) as promotor Breast Cancer July 2015 Phase 1
    NCT01948141 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim Recurrent Non-small Cell Lung Cancer|Squamous Cell Lung Cancer|Stage III Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer January 30, 2014 Phase 2
    NCT02009579 Belgian Gynaecological Oncology Group|Grupo Español de Investigación en Cáncer de Ovario|Mario Negri Gynecologic Oncology group (MANGO)|Multicenter Italian Trials in Ovarian Cancer (MITO)|Institute of Cancer Research, United Kingdom|North Eastern Germany Society of Gynaecologic Oncology Uterine Cervical Neoplasms March 2014 Phase 2
    NCT02496585 Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim Lung Cancer|Lung Metastases July 2015 Phase 2
    NCT01225887 Gynecologic Oncology Group|National Cancer Institute (NCI) Endometrial Adenocarcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Mucinous Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Squamous Cell Carcinoma|Endometrial Transitional Cell Carcinoma|Endometrial Undifferentiated Carcinoma|Malignant Uterine Corpus Mixed Epithelial and Mesenchymal Neoplasm|Recurrent Uterine Corpus Carcinoma October 2011 Phase 2
    NCT02300298 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2014 Phase 1
    NCT01658462 Centre Oscar Lambret|Boehringer Ingelheim Breast Cancer May 2013 Phase 2
    NCT02393755 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim|National Comprehensive Cancer Network Colon Adenocarcinoma|Rectal Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer May 8, 2015 Phase 1|Phase 2
    NCT02191865 Boehringer Ingelheim Hepatic Insufficiency July 2014 Phase 1
    NCT02730416 Nordic Society for Gynaecologic Oncology|North Eastern Germany Society of Gynaecologic Oncology|Belgian Gynaecological Oncology Group|ARCAGY/ GINECO GROUP Endometrial Cancer November 2016 Phase 2
    NCT02665143 Yale University|Vanderbilt University Medical Center Relapsed/Refractory Acute Myeloid Leukemia June 2016 Phase 1|Phase 2
    NCT02863055 European Organisation for Research and Treatment of Cancer - EORTC Malignant Pleural Mesothelioma February 2017 Phase 2
    NCT02399215 Roswell Park Cancer Institute|National Cancer Institute (NCI) Carcinoid Tumor|Metastatic Carcinoid Tumor|Neuroendocrine Neoplasm May 15, 2015 Phase 2
    NCT02597933 Boehringer Ingelheim Scleroderma, Systemic November 12, 2015 Phase 3
    NCT02606877 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis April 19, 2016 Phase 4
    NCT02751385 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung May 20, 2016 Phase 1
    NCT02856425 Gustave Roussy, Cancer Campus, Grand Paris Patients With Any Advanced Solid Tumors. July 2016 Phase 1
    NCT02780700 Boehringer Ingelheim Colorectal Neoplasms July 5, 2016 Phase 2
    NCT02999178 Boehringer Ingelheim Lung Diseases, Interstitial January 17, 2017 Phase 3
    NCT02452463 Roswell Park Cancer Institute|National Cancer Institute (NCI)|National Comprehensive Cancer Network Radiation-Induced Pneumonitis|Stage IIA Non-Small Cell Lung Carcinoma|Stage IIB Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer June 29, 2015 Phase 2
    NCT02668393 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 7, 2016 Phase 1
    NCT01979952 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis November 26, 2013 Phase 3
    NCT02866370 NHS Greater Glasgow and Clyde|Boehringer Ingelheim|Cancer Research UK|European Organisation for Research and Treatment of Cancer - EORTC|Nordic Society for Gynaecologic Oncology|ARCAGY/ GINECO GROUP Ovarian Clear Cell Carcinoma|Endometrial Clear Cell Carcinoma April 2015 Phase 2
    NCT02230982 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis February 2015
    NCT02788474 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis June 9, 2016 Phase 4
    NCT02171156 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis
    NCT01770392 Boehringer Ingelheim Healthy January 2013 Phase 1
    NCT02607722 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis August 31, 2015
    NCT02231164 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2014 Phase 3
    NCT02856867 European Organisation for Research and Treatment of Cancer - EORTC Esophagogastric Adenocarcinoma|Metastatic Disease|No Previous Chemotherapy for Metastatic Esophagogastric Cancer December 2016 Phase 2
    NCT02802345 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis June 30, 2016 Phase 3
    NCT01679613 Boehringer Ingelheim Healthy September 2012 Phase 1
    NCT01907100 Boehringer Ingelheim Mesothelioma September 19, 2013 Phase 3
    NCT01594125 Boehringer Ingelheim Carcinoma, Hepatocellular May 2012 Phase 1
    NCT01417156 Boehringer Ingelheim Pulmonary Fibrosis September 2011 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 1.8532 mL 9.2658 mL 18.5316 mL
    5 mM 0.3706 mL 1.8532 mL 3.7063 mL
    10 mM 0.1853 mL 0.9266 mL 1.8532 mL
    Kinase Assay
    [2]

    Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    BIBF 1120 is formulated in a 0.5 % Natrosol solution.

    Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×106 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×106 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    539.62

    Formula

    C₃₁H₃₃N₅O₄

    CAS No.

    656247-17-5

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    BIBF 1120 (Nintedanib) is prepared in vehicle solution that consists of 0.5% HPMC solution[3].

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

    References

    Purity: 99.72%

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    BIBF 1120
    Cat. No.:
    HY-50904
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