1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Autophagy
  2. EGFR
    Autophagy

Afatinib (Synonyms: BIBW 2992)

Cat. No.: HY-10261 Purity: 99.58%
Data Sheet SDS Handling Instructions

Afatinib is an irreversible, dual EGFR/HER2 inhibitor, shows potent activity against wild-type and mutant forms of EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

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

Afatinib Chemical Structure

CAS No. : 850140-72-6

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Other Forms of Afatinib:

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Description

Afatinib is an irreversible, dual EGFR/HER2 inhibitor, shows potent activity against wild-type and mutant forms of EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

IC50 & Target

IC50: 0.5 nM (EGFRwt), 0.4 nM (EGFRL858R), 10 nM (EGFRL858R/T790M), 14 nM (HER2)[1]

In Vitro

In cell-free in vitro kinase assays, Afatinib (BIBW2992) dimaleate shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to Gefitinib in potency for L858R EGFR, but about 100-fold more active against the Gefitinib-resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 is furthermore comparable to Lapatinib and Canertinib for in vitro potency against HER2, with an IC50 of 14 nM. The most sensitive kinase in this evaluation is lyn with an IC50 of 736 nM[1]. Afatinib is an irreversible inhibitor of these ErbB family receptors. Esophageal squamous cell carcinoma (ESCC) cell lines are sensitive to Afatinib with IC50 concentrations at lower micro-molar range (at 48 hour incubation: HKESC-1=78 nM, HKESC-2=115 nM, KYSE510=3.182 μM, SLMT-1=4.625 μM and EC-1=1.489 μM; and at 72 hour incubation: HKESC-1=2 nM, HKESC-2=2 nM, KYSE510=1.090 μM, SLMT-1=1.161 μM and EC-1=109 nM) with a maximum growth inhibition over 95%. Afatinib can strongly induce G0/G1 cell cycle arrest in HKESC-2 and EC-1 in a dose- and time-dependent manner[2].

In Vivo

Afatinib (15 mg/kg) strongly inhibits the growth of HKESC-2 tumor once the treatment began. Average tumor sizes of vehicle and treatment at end point are 348±24 mm3 and 108±36 mm3 respectively, showing significantly difference between them. And apparently tumor size does not bounce back in a short period of time after the end of Afatinib administration. Without rapid change of body weight throughout the treatment shows that the toxicity of Afatinib is minimal and this drug is well tolerated[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02423525 Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute Brain Cancer December 2016 Phase 1
NCT03083678 Leiden University Medical Center|Chordoma Foundation|Boehringer Ingelheim Chordoma June 2017 Phase 2
NCT01953913 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung September 30, 2013 Phase 3
NCT01522768 Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim|University of Southern California|Dana-Farber Cancer Institute|United States Department of Defense Esophageal Cancer|Gastric Cancer March 2012 Phase 2
NCT02511847 National Taiwan University Hospital Triple Negative Breast Cancer August 2015 Phase 2
NCT01320280 Universitätsklinikum Hamburg-Eppendorf|Boehringer Ingelheim Refractory Cancer May 2011 Phase 2
NCT02514174 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|ErbB Receptors August 18, 2015 Phase 4
NCT02491099 Yale University|Boehringer Ingelheim HER2/Neu+ Uterine Serous Carcinoma June 2015 Phase 2
NCT02096718 Boehringer Ingelheim Renal Insufficiency May 2014 Phase 1
NCT02625168 The University of Hong Kong Lung Cancer January 2013 Phase 2
NCT02629523 Chonnam National University Hospital Lung Neoplasms|EGFR Gene Mutation June 2016 Phase 2
NCT02208843 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2, 2014 Phase 4
NCT02122172 University of Chicago|National Cancer Institute (NCI) Distal Urethral Cancer|Proximal Urethral Cancer|Recurrent Bladder Cancer|Recurrent Urethral Cancer|Stage III Bladder Cancer|Stage III Urethral Cancer|Stage IV Bladder Cancer|Stage IV Urethral Cancer|Ureter Cancer October 2013 Phase 2
NCT01853826 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung July 17, 2013 Phase 3
NCT01415011 University College, London|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2012 Phase 2
NCT01415674 UNICANCER Carcinoma, Squamous Cell of Head and Neck January 2012 Phase 2
NCT02364609 University of California, Davis|National Cancer Institute (NCI) Recurrent 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 September 2015 Phase 1
NCT01538381 European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim Carcinoma, Squamous Cell of Head and Neck July 2012 Phase 2
NCT02369484 European Thoracic Oncology Platform NSCLC June 2015 Phase 2
NCT02501603 Yonsei University Gastric Cancer|Gastroesophageal Junction Cancer July 2016 Phase 2
NCT02274012 Columbia University|Boehringer Ingelheim HER-2 Positive Gastric Cancer|Gastrooesophageal Cancer|Esophageal Cancer May 29, 2014 Phase 2
NCT01824823 ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group Head and Neck Squamous Cell Carcinoma July 2013 Phase 2
NCT01746251 Massachusetts General Hospital|National Comprehensive Cancer Network Non Small Cell Lung Cancer January 2013 Phase 2
NCT01783587 Dana-Farber Cancer Institute|National Comprehensive Cancer Network Squamous Cell Carcinoma of the Head and Neck February 2013 Phase 1
NCT02044380 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2014 Phase 3
NCT02191891 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 21, 2014 Phase 1
NCT01325428 Boehringer Ingelheim Breast Neoplasms August 2011 Phase 2
NCT01480141 Medical University of South Carolina|Boehringer Ingelheim Lung Cancer January 2012 Phase 2
NCT01427478 Centre Leon Berard|Boehringer Ingelheim Head and Neck Squamous Cell Carcinoma September 2011 Phase 3
NCT01466660 Boehringer Ingelheim Lung Neoplasms December 2011 Phase 2
NCT02979977 Yale University|National Comprehensive Cancer Network|Boehringer Ingelheim Squamous Cell Cancers of the Head and Neck March 24, 2017 Phase 2
NCT02451553 University of Washington|National Cancer Institute (NCI) Bile Duct Carcinoma|Recurrent Pancreatic Carcinoma|Solid Neoplasm|Stage III Pancreatic Cancer|Stage IVA Pancreatic Cancer|Stage IVB Pancreatic Cancer November 5, 2015 Phase 1
NCT01743365 Hellenic Cooperative Oncology Group|Boehringer Ingelheim Gastric Cancer|Gastroesophageal Junction Cancer January 2013 Phase 2
NCT02470065 European Organisation for Research and Treatment of Cancer - EORTC Non Small Cell Lung Cancer January 2016 Phase 2
NCT02975141 PD Dr. med. Volker Heinemann|Technische Universität München|University of Cologne|Ludwig-Maximilians - University of Munich Metastatic Pancreatic Cancer September 2016 Phase 1
NCT02695290 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|ErbB Receptors March 17, 2016 Phase 4
NCT02876081 Groupe Hospitalier Paris Saint Joseph SMALL CELL LUNG CARCINOMA December 2016 Phase 2
NCT02716311 Intergroupe Francophone de Cancerologie Thoracique Non Small Cell Lung Cancer May 2016 Phase 2
NCT01721525 Memorial Sloan Kettering Cancer Center|National Comprehensive Cancer Network|Boehringer Ingelheim Head and Neck Cancer|Squamous Cell Cancer November 2012 Phase 1
NCT02183883 University College, London|Boehringer Ingelheim Non-small Cell Lung Cancer December 2016 Phase 2
NCT01814553 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2013 Phase 3
NCT01919879 UNICANCER Metastatic Colorectal Cancer October 2012 Phase 2
NCT02780687 Boehringer Ingelheim Urologic Neoplasms June 9, 2016 Phase 2
NCT01836341 Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim|National Comprehensive Cancer Network Non-small Cell Lung Cancer April 2013 Phase 1
NCT02438722 Southwest Oncology Group|National Cancer Institute (NCI) Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer March 2015 Phase 2|Phase 3
NCT01932229 Sheba Medical Center NSCLC February 2013 Phase 2
NCT01861223 Samsung Medical Center NSCLC May 2013 Phase 1|Phase 2
NCT01553942 Massachusetts General Hospital Lung Cancer April 2012 Phase 2
NCT01251653 Boehringer Ingelheim Neoplasms November 2010
NCT01298063 Boehringer Ingelheim Liver Diseases|Healthy February 2011 Phase 1
NCT01426958 Boehringer Ingelheim Healthy August 2011 Phase 1
NCT01396265 Boehringer Ingelheim Healthy July 2011 Phase 1
NCT01271725 Boehringer Ingelheim Breast Neoplasms May 24, 2011 Phase 2
NCT02597946 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 18, 2016 Phase 2
NCT01214616 Boehringer Ingelheim Neoplasms October 2010 Phase 1
NCT00748709 Boehringer Ingelheim Neoplasms October 2008 Phase 2
NCT02768337 Cambridge University Hospitals NHS Foundation Trust|Boehringer Ingelheim|Cancer Research UK|University of Cambridge|The Brain Tumour Charity Lung Cancer|Breast Cancer|Brain Cancer|Advanced Breast Cancer|Advanced Lung Cancer February 2015 Phase 1|Phase 2
NCT02216617 Groupe Oncologie Radiotherapie Tete et Cou HNSCC August 2014 Phase 1
NCT02506517 University Health Network, Toronto|Boehringer Ingelheim Solid Tumors August 2015 Phase 2
NCT02450656 The Netherlands Cancer Institute|AstraZeneca|Boehringer Ingelheim Colorectal Neoplasms|Gastrointestinal Neoplasms|Pancreatic Neoplasms|Carcinoma, Non-Small-Cell Lung June 2015 Phase 1|Phase 2
NCT01523587 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 5, 2012 Phase 3
NCT01441596 Boehringer Ingelheim Breast Neoplasms|Neoplasm Metastasis October 2011 Phase 2
NCT02020577 Boehringer Ingelheim Neoplasms December 2013 Phase 1
NCT03157089 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 15, 2017 Phase 2
NCT01649284 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung July 2012
NCT01649271 Boehringer Ingelheim Breast Neoplasms|Stomach Neoplasms July 2012 Phase 1
NCT02372006 Boehringer Ingelheim Neuroectodermal Tumors|Rhabdomyosarcoma April 29, 2015 Phase 1
NCT01856478 Boehringer Ingelheim Head and Neck Neoplasms May 23, 2013 Phase 3
NCT02145637 Yonsei University NSCLC July 2014 Phase 1
NCT01345682 Boehringer Ingelheim Head and Neck Neoplasms|Carcinoma, Squamous Cell January 5, 2012 Phase 3
NCT02131155 Boehringer Ingelheim Head and Neck Neoplasms July 2014 Phase 3
NCT01345669 Boehringer Ingelheim Head and Neck Neoplasms October 2011 Phase 3
NCT02115048 Translational Research in Oncology|Boehringer Ingelheim Breast Neoplasms July 2014 Phase 2
NCT01931306 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung
NCT03054038 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Non-Small Cell Lung Carcinoma August 2017 Phase 1
NCT01999985 H. Lee Moffitt Cancer Center and Research Institute|Boehringer Ingelheim|Bristol-Myers Squibb Lung Cancer|Non-small Cell Lung Cancer (NSCLC) December 31, 2013 Phase 1
NCT01732640 Sidney Kimmel Comprehensive Cancer Center|Vanderbilt-Ingram Cancer Center|National Comprehensive Cancer Network Squamous Cell Carcinoma of the Head and Neck December 2012 Phase 1|Phase 2
NCT01003899 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 2
NCT01594177 German Breast Group|Boehringer Ingelheim Unilateral HER2 Positive Breast Cancer May 2012 Phase 2
NCT02047903 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2014
NCT01728818 PD Dr. med. Volker Heinemann|Boehringer Ingelheim|Ludwig-Maximilians - University of Munich Focus of Study Instead April 2013 Phase 2
NCT02488694 AIO-Studien-gGmbH|Boehringer Ingelheim Non-small-cell Lung Cancer With Somatic EGFR Mutations November 2015 Phase 2
NCT02131259 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung May 7, 2014
NCT02795156 SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma September 28, 2016 Phase 2
NCT01776684 Samsung Medical Center|AstraZeneca EGFR Mutation Positive Non-small Cell Lung Cancer June 2012
NCT03088059 European Organisation for Research and Treatment of Cancer - EORTC Carcinoma, Squamous Cell of Head and Neck July 2017 Phase 2
NCT02465060 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cer August 12, 2015 Phase 2
NCT00431067 Boehringer Ingelheim Breast Neoplasms September 2006 Phase 2
NCT00525148 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 2007 Phase 2
NCT01679405 Johannes Gutenberg University Mainz Metastatic Disease August 2012 Phase 1
NCT02171702 Boehringer Ingelheim Neoplasms November 2004 Phase 1
NCT01206816 Boehringer Ingelheim Neoplasms October 2010 Phase 1
NCT02171637 Boehringer Ingelheim Neoplasms November 2003 Phase 1
NCT02171728 Boehringer Ingelheim Neoplasms November 2004 Phase 1
NCT00796549 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2008 Phase 2
NCT00716417 Boehringer Ingelheim Neoplasms July 2008 Phase 1
NCT00875433 Boehringer Ingelheim Neoplasms March 2009 Phase 2
NCT00711594 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2008 Phase 2
NCT02171650 Boehringer Ingelheim Neoplasms December 2004 Phase 1
NCT01156545 National Cancer Center, Korea|Boehringer Ingelheim Non-small Cell Lung Cancer October 2010 Phase 2
NCT01542437 Instituto Nacional de Cancerologia de Mexico Non-Small Cell Lung Cancer|EGFR|HER-2 January 2012 Phase 2
NCT01152437 Boehringer Ingelheim Colorectal Neoplasms June 2010 Phase 2
NCT00727506 Boehringer Ingelheim Glioma July 2008 Phase 2
NCT02171754 Boehringer Ingelheim Healthy September 2009 Phase 1
NCT02171741 Boehringer Ingelheim Neoplasms April 2005 Phase 1
NCT00950742 Boehringer Ingelheim Breast Neoplasms August 2009 Phase 1
NCT00425854 Boehringer Ingelheim Breast Neoplasms November 2006 Phase 2
NCT00998296 Boehringer Ingelheim Neoplasms October 2009 Phase 1
NCT00993499 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 1
NCT00708214 Boehringer Ingelheim Breast Neoplasms January 2007 Phase 2
NCT01121393 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|Adenocarcinoma April 19, 2010 Phase 3
NCT00949650 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|Adenocarcinoma August 2009 Phase 3
NCT00656136 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2008 Phase 3
NCT02171689 Boehringer Ingelheim Healthy July 2006 Phase 1
NCT01531764 University of Magdeburg|Boehringer Ingelheim Carcinoma Breast Stage IV July 2012 Phase 2
NCT00730821 Boehringer Ingelheim Neoplasms January 2007 Phase 1
NCT02171767 Boehringer Ingelheim Healthy August 2009 Phase 1
NCT02171676 Boehringer Ingelheim Neoplasms May 2005 Phase 1
NCT00826267 Boehringer Ingelheim Breast Neoplasms January 2009 Phase 2
NCT02171663 Boehringer Ingelheim Neoplasms March 2004 Phase 1
NCT00514943 Boehringer Ingelheim Head and Neck Neoplasms|Carcinoma, Squamous Cell August 2007 Phase 2
NCT01074177 Massachusetts General Hospital|University of Texas|Boehringer Ingelheim Non-small Cell Lung Cancer|EGFR Mutations February 2011
NCT01125566 Boehringer Ingelheim Breast Neoplasms June 2010 Phase 3
NCT01090011 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2010 Phase 1
NCT02171715 Boehringer Ingelheim Healthy January 2009 Phase 1
NCT00801294 Boehringer Ingelheim Colorectal Neoplasms July 2006 Phase 2
NCT01169675 Boehringer Ingelheim Neoplasms July 2010 Phase 1
NCT01085136 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung February 2010 Phase 3
NCT00706628 Boehringer Ingelheim Prostatic Neoplasms March 2006 Phase 2
NCT02271906 M.D. Anderson Cancer Center|Boehringer Ingelheim Lung Cancer July 2015 Phase 2
NCT00809133 Boehringer Ingelheim Neoplasms May 2007 Phase 1
NCT01209650 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung
NCT00906698 Boehringer Ingelheim Neoplasms June 2009 Phase 1
NCT00730925 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung June 2008 Phase 2
NCT00977431 Boehringer Ingelheim Glioblastoma September 17, 2009 Phase 1
NCT02353936 Yonsei University Squamous Cell Carcinoma of Esophagus January 2015 Phase 2
NCT02423525 Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute Brain Cancer December 2016 Phase 1
NCT03083678 Leiden University Medical Center|Chordoma Foundation|Boehringer Ingelheim Chordoma June 2017 Phase 2
NCT01953913 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung September 30, 2013 Phase 3
NCT01522768 Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim|University of Southern California|Dana-Farber Cancer Institute|United States Department of Defense Esophageal Cancer|Gastric Cancer March 2012 Phase 2
NCT02511847 National Taiwan University Hospital Triple Negative Breast Cancer August 2015 Phase 2
NCT01320280 Universitätsklinikum Hamburg-Eppendorf|Boehringer Ingelheim Refractory Cancer May 2011 Phase 2
NCT02514174 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|ErbB Receptors August 18, 2015 Phase 4
NCT02491099 Yale University|Boehringer Ingelheim HER2/Neu+ Uterine Serous Carcinoma June 2015 Phase 2
NCT02096718 Boehringer Ingelheim Renal Insufficiency May 2014 Phase 1
NCT02625168 The University of Hong Kong Lung Cancer January 2013 Phase 2
NCT02629523 Chonnam National University Hospital Lung Neoplasms|EGFR Gene Mutation June 2016 Phase 2
NCT02208843 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2, 2014 Phase 4
NCT02122172 University of Chicago|National Cancer Institute (NCI) Distal Urethral Cancer|Proximal Urethral Cancer|Recurrent Bladder Cancer|Recurrent Urethral Cancer|Stage III Bladder Cancer|Stage III Urethral Cancer|Stage IV Bladder Cancer|Stage IV Urethral Cancer|Ureter Cancer October 2013 Phase 2
NCT01853826 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung July 17, 2013 Phase 3
NCT01415011 University College, London|Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2012 Phase 2
NCT01415674 UNICANCER Carcinoma, Squamous Cell of Head and Neck January 2012 Phase 2
NCT02364609 University of California, Davis|National Cancer Institute (NCI) Recurrent 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 September 2015 Phase 1
NCT01538381 European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim Carcinoma, Squamous Cell of Head and Neck July 2012 Phase 2
NCT02369484 European Thoracic Oncology Platform NSCLC June 2015 Phase 2
NCT02501603 Yonsei University Gastric Cancer|Gastroesophageal Junction Cancer July 2016 Phase 2
NCT02274012 Columbia University|Boehringer Ingelheim HER-2 Positive Gastric Cancer|Gastrooesophageal Cancer|Esophageal Cancer May 29, 2014 Phase 2
NCT01824823 ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group Head and Neck Squamous Cell Carcinoma July 2013 Phase 2
NCT01746251 Massachusetts General Hospital|National Comprehensive Cancer Network Non Small Cell Lung Cancer January 2013 Phase 2
NCT01783587 Dana-Farber Cancer Institute|National Comprehensive Cancer Network Squamous Cell Carcinoma of the Head and Neck February 2013 Phase 1
NCT02044380 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2014 Phase 3
NCT02191891 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 21, 2014 Phase 1
NCT01325428 Boehringer Ingelheim Breast Neoplasms August 2011 Phase 2
NCT01480141 Medical University of South Carolina|Boehringer Ingelheim Lung Cancer January 2012 Phase 2
NCT01427478 Centre Leon Berard|Boehringer Ingelheim Head and Neck Squamous Cell Carcinoma September 2011 Phase 3
NCT01466660 Boehringer Ingelheim Lung Neoplasms December 2011 Phase 2
NCT02979977 Yale University|National Comprehensive Cancer Network|Boehringer Ingelheim Squamous Cell Cancers of the Head and Neck March 24, 2017 Phase 2
NCT02451553 University of Washington|National Cancer Institute (NCI) Bile Duct Carcinoma|Recurrent Pancreatic Carcinoma|Solid Neoplasm|Stage III Pancreatic Cancer|Stage IVA Pancreatic Cancer|Stage IVB Pancreatic Cancer November 5, 2015 Phase 1
NCT01743365 Hellenic Cooperative Oncology Group|Boehringer Ingelheim Gastric Cancer|Gastroesophageal Junction Cancer January 2013 Phase 2
NCT02470065 European Organisation for Research and Treatment of Cancer - EORTC Non Small Cell Lung Cancer January 2016 Phase 2
NCT02975141 PD Dr. med. Volker Heinemann|Technische Universität München|University of Cologne|Ludwig-Maximilians - University of Munich Metastatic Pancreatic Cancer September 2016 Phase 1
NCT02695290 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung|ErbB Receptors March 17, 2016 Phase 4
NCT02876081 Groupe Hospitalier Paris Saint Joseph SMALL CELL LUNG CARCINOMA December 2016 Phase 2
NCT02716311 Intergroupe Francophone de Cancerologie Thoracique Non Small Cell Lung Cancer May 2016 Phase 2
NCT01721525 Memorial Sloan Kettering Cancer Center|National Comprehensive Cancer Network|Boehringer Ingelheim Head and Neck Cancer|Squamous Cell Cancer November 2012 Phase 1
NCT02183883 University College, London|Boehringer Ingelheim Non-small Cell Lung Cancer December 2016 Phase 2
NCT01814553 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2013 Phase 3
NCT01919879 UNICANCER Metastatic Colorectal Cancer October 2012 Phase 2
NCT02780687 Boehringer Ingelheim Urologic Neoplasms June 9, 2016 Phase 2
NCT01836341 Memorial Sloan Kettering Cancer Center|Boehringer Ingelheim|National Comprehensive Cancer Network Non-small Cell Lung Cancer April 2013 Phase 1
NCT02438722 Southwest Oncology Group|National Cancer Institute (NCI) Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer March 2015 Phase 2|Phase 3
NCT01932229 Sheba Medical Center NSCLC February 2013 Phase 2
NCT01861223 Samsung Medical Center NSCLC May 2013 Phase 1|Phase 2
NCT01553942 Massachusetts General Hospital Lung Cancer April 2012 Phase 2
NCT01251653 Boehringer Ingelheim Neoplasms November 2010
NCT01298063 Boehringer Ingelheim Liver Diseases|Healthy February 2011 Phase 1
NCT01426958 Boehringer Ingelheim Healthy August 2011 Phase 1
NCT01396265 Boehringer Ingelheim Healthy July 2011 Phase 1
NCT01271725 Boehringer Ingelheim Breast Neoplasms May 24, 2011 Phase 2
NCT02597946 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 18, 2016 Phase 2
NCT01214616 Boehringer Ingelheim Neoplasms October 2010 Phase 1
NCT00748709 Boehringer Ingelheim Neoplasms October 2008 Phase 2
NCT02768337 Cambridge University Hospitals NHS Foundation Trust|Boehringer Ingelheim|Cancer Research UK|University of Cambridge|The Brain Tumour Charity Lung Cancer|Breast Cancer|Brain Cancer|Advanced Breast Cancer|Advanced Lung Cancer February 2015 Phase 1|Phase 2
NCT02216617 Groupe Oncologie Radiotherapie Tete et Cou HNSCC August 2014 Phase 1
NCT02506517 University Health Network, Toronto|Boehringer Ingelheim Solid Tumors August 2015 Phase 2
NCT02450656 The Netherlands Cancer Institute|AstraZeneca|Boehringer Ingelheim Colorectal Neoplasms|Gastrointestinal Neoplasms|Pancreatic Neoplasms|Carcinoma, Non-Small-Cell Lung June 2015 Phase 1|Phase 2
NCT01523587 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 5, 2012 Phase 3
NCT01441596 Boehringer Ingelheim Breast Neoplasms|Neoplasm Metastasis October 2011 Phase 2
NCT02020577 Boehringer Ingelheim Neoplasms December 2013 Phase 1
NCT03157089 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 15, 2017 Phase 2
NCT01649284 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung July 2012
NCT01649271 Boehringer Ingelheim Breast Neoplasms|Stomach Neoplasms July 2012 Phase 1
NCT02372006 Boehringer Ingelheim Neuroectodermal Tumors|Rhabdomyosarcoma April 29, 2015 Phase 1
NCT01856478 Boehringer Ingelheim Head and Neck Neoplasms May 23, 2013 Phase 3
NCT02145637 Yonsei University NSCLC July 2014 Phase 1
NCT01345682 Boehringer Ingelheim Head and Neck Neoplasms|Carcinoma, Squamous Cell January 5, 2012 Phase 3
NCT02131155 Boehringer Ingelheim Head and Neck Neoplasms July 2014 Phase 3
NCT01345669 Boehringer Ingelheim Head and Neck Neoplasms October 2011 Phase 3
NCT02115048 Translational Research in Oncology|Boehringer Ingelheim Breast Neoplasms July 2014 Phase 2
NCT01931306 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung
NCT03054038 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Non-Small Cell Lung Carcinoma August 2017 Phase 1
NCT01999985 H. Lee Moffitt Cancer Center and Research Institute|Boehringer Ingelheim|Bristol-Myers Squibb Lung Cancer|Non-small Cell Lung Cancer (NSCLC) December 31, 2013 Phase 1
NCT01732640 Sidney Kimmel Comprehensive Cancer Center|Vanderbilt-Ingram Cancer Center|National Comprehensive Cancer Network Squamous Cell Carcinoma of the Head and Neck December 2012 Phase 1|Phase 2
NCT01003899 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 2
NCT01594177 German Breast Group|Boehringer Ingelheim Unilateral HER2 Positive Breast Cancer May 2012 Phase 2
NCT02047903 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung March 2014
NCT01728818 PD Dr. med. Volker Heinemann|Boehringer Ingelheim|Ludwig-Maximilians - University of Munich Focus of Study Instead April 2013 Phase 2
NCT02488694 AIO-Studien-gGmbH|Boehringer Ingelheim Non-small-cell Lung Cancer With Somatic EGFR Mutations November 2015 Phase 2
NCT02131259 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung May 7, 2014
NCT02795156 SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma September 28, 2016 Phase 2
NCT01776684 Samsung Medical Center|AstraZeneca EGFR Mutation Positive Non-small Cell Lung Cancer June 2012
NCT03088059 European Organisation for Research and Treatment of Cancer - EORTC Carcinoma, Squamous Cell of Head and Neck July 2017 Phase 2
NCT02465060 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cer August 12, 2015 Phase 2
NCT00431067 Boehringer Ingelheim Breast Neoplasms September 2006 Phase 2
NCT00525148 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung August 2007 Phase 2
NCT01679405 Johannes Gutenberg University Mainz Metastatic Disease August 2012 Phase 1
NCT02171702 Boehringer Ingelheim Neoplasms November 2004 Phase 1
NCT01206816 Boehringer Ingelheim Neoplasms October 2010 Phase 1
NCT02171637 Boehringer Ingelheim Neoplasms November 2003 Phase 1
NCT02171728 Boehringer Ingelheim Neoplasms November 2004 Phase 1
NCT00796549 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung December 2008 Phase 2
NCT00716417 Boehringer Ingelheim Neoplasms July 2008 Phase 1
NCT00875433 Boehringer Ingelheim Neoplasms March 2009 Phase 2
NCT00711594 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung April 2008 Phase 2
NCT02171650 Boehringer Ingelheim Neoplasms December 2004 Phase 1
NCT01156545 National Cancer Center, Korea|Boehringer Ingelheim Non-small Cell Lung Cancer October 2010 Phase 2
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NCT00993499 Boehringer Ingelheim Carcinoma, Non-Small-Cell Lung October 2009 Phase 1
NCT00708214 Boehringer Ingelheim Breast Neoplasms January 2007 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.0579 mL 10.2893 mL 20.5787 mL
5 mM 0.4116 mL 2.0579 mL 4.1157 mL
10 mM 0.2058 mL 1.0289 mL 2.0579 mL
Kinase Assay
[1]

The EGFR kinase domain-GST fusion proteins are extracted from Sf9 biomasses, 72 hours post infection, with HEPEX (20 mM HEPES pH 7.4, 100 mM NaCl, 10 mM β-glycerophosphate, 10 mM para-nitro-phenylphosphate, 30 mM NaF, 5 mM EDTA, 5% glycerol, 1% Triton X-100, 1 mM Na3VO4, 0.1% SDS, 0.5 µg/mL pepstatin A, aprotinin 20 KIU/mL, Leupeptin 2 µg/mL, Benzamidine 1 mM, 2.5 μg/mL 3,4-dichloroisocoumarin, 2.5 μg/mL trans-epoxysuccinyl-L-leucyl-L-amido butane and 0.002% PMSF) and used for the determination of the IC50 values. Each 100 µL enzyme reaction contains 10 μL of Afatinib (BIBW2992) in 50 % Me2SO, 20 μL of substrate solution (200 mM HEPES pH 7.4, 50 mM Mg-acetate, 2.5 mg/mL poly (EY), 5 μg/mL bio-pEY) and 20 µL enzyme preparation. The enzymatic reaction is started by addition of 50 µL of a 100 µM ATP solution made in 10 mM MgCl2. Assays are carried out at room temperature for 30 minutes and terminated by the addition of 50 µL of stop solution (250 mM EDTA in 20 mM HEPES pH 7.4). 100 µL are transferred to a streptavidin coated microtiterplate, after an incubation time of 60 min at room temperature the plate is washed with 200 µL of wash solution (50 mM Tris, 0.05% Tween20). A 100 µL aliquot of a HRPO- labeled anti-PY antibody (PY20H Anti-Ptyr:HRP) 250 ng/mL are added to the wells. After 60 min of incubation, the plate is washed three times with a 200 µL wash solution. The samples are then developed with a 100 µL TMB Peroxidase Solution (A:B=1:1). The reaction is stopped after 10 min. The plate is transferred to an ELISA reader and extinction is measured at OD450nm. All data points are performed in triplicates[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Afatinib is dissolved in DMSO (100 mM) and stored (-80°C), and then diluted in corresponding medium just before addition to cell cultures[2].

Human ESCC cell lines, EC-1, HKESC1 and HKESC2, SLMT1, and KYSE510 are cultured in RPMI with 10% fetal bovine serum (FBS). Cytotoxicity is assessed by a colorimetric assay using MTT. Tumour cells are cultured in 48-well plates (3000-8000 cells per well) in respective culture medium. Afatinib in complete medium is added at 24 hr after cell plating and incubated at 37°C with 5% CO2 for 48 and 72 hr. Cell growth inhibition is expressed as the percentage of absorbance of control cultures measured at 570 nm with a microplate reader and 50% of the maximum growth inhibition (IC50) is calculated by GraphPad PRISM. In each experiment, triplicate wells are performed for each drug concentration (n=3), and assay is repeated in three independent experiments[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Afatinib is dissolved in 0.5% methylcellulose (Mice)[2].

Mice[2]
Six weeks old female athymic nude mice (nu/nu) weighing about 16-20 gram are used. ESCC xenografts are established by inoculating HKESC-2 (6×104 cells re-suspended in 50 μL of HBSS-buffer) subcutaneously into both flanks of the nude mice. When tumor size reached to 4-6 mm diameter, they are randomized in either treatment (15 mg/kg) or vehicle control group. Afatinib for treatment is prepared by dissolving in 0.5% methylcellulose before administration. Either drug or vehicle is administered to mouse by oral gavage in a schedule of 5 days on plus 2 days off for two weeks. Drug efficacy is evaluated by monitoring the change in tumor size with caliper. Tumor volume is calculated with the formula Tumor Volume=(width2×length)/2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

485.94

Formula

C₂₄H₂₅ClFN₅O₃

CAS No.

850140-72-6

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: 99.58%

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Afatinib
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