Page last updated: 2024-09-03

gefitinib and ekb 569

gefitinib has been researched along with ekb 569 in 24 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(ekb 569)
Trials
(ekb 569)
Recent Studies (post-2010) (ekb 569)
5,2315662,91968533

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)ekb 569 (IC50)
Epidermal growth factor receptorHomo sapiens (human)0.0489
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)1.2298
Vascular endothelial growth factor receptor 2Homo sapiens (human)3.131
Serine/threonine-protein kinase Nek2Homo sapiens (human)0.661

Research

Studies (24)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's12 (50.00)29.6817
2010's12 (50.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Brawner Floyd, MB; Greenberger, LM; Nilakantan, R; Rabindran, SK; Shen, R; Tsou, HR; Wang, YF; Wissner, A1
Atteridge, CE; Azimioara, MD; Benedetti, MG; Biggs, WH; Carter, TA; Ciceri, P; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Galvin, M; Gerlach, JL; Grotzfeld, RM; Herrgard, S; Insko, DE; Insko, MA; Lai, AG; Lélias, JM; Lockhart, DJ; Mehta, SA; Milanov, ZV; Patel, HK; Treiber, DK; Velasco, AM; Wodicka, LM; Zarrinkar, PP1
Cheung, K; Dushin, RG; Floyd, MB; Fraser, HL; Ingalls, CL; Loganzo, F; Nittoli, T; Ravi, MR; Tan, X; Wissner, A1
Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Russu, WA; Shallal, HM1
Anderton, MJ; Ashton, S; Bethel, PA; Box, M; Butterworth, S; Chorley, CG; Chuaqui, C; Colclough, N; Cross, DA; Dakin, LA; Debreczeni, JÉ; Eberlein, C; Finlay, MR; Grist, M; Hill, GB; Klinowska, TC; Lane, C; Martin, S; Orme, JP; Smith, P; Wang, F; Ward, RA; Waring, MJ1
Barouch-Bentov, R; Bekerman, E; Chaikuad, A; Chang, L; De Jonghe, S; Einav, S; Herdewijn, P; Heroven, C; Knapp, S; Kovackova, S; Neveu, G; Šála, M1
Abou El Ella, DA; Aly, RM; El-Motwally, AM; Ibrahim, DA1
Bantscheff, M; Bergamini, G; Gohlke, B; Gupta, V; Handa, H; Heinzlmeir, S; Helm, D; Klaeger, S; Kuster, B; Médard, G; Perrin, J; Preissner, R; Qiao, H; Savitski, MM1
Althaus, IW; Black, SL; Blaser, A; Bridges, A; Denny, WA; Ellis, PA; Ellis, T; Fakhoury, S; Gonzales, AJ; Harvey, PJ; Hook, K; Lee, H; McCarthy, FO; Palmer, BD; Reed, JE; Rivault, F; Schlosser, K; Sexton, K; Smaill, JB; Spicer, JA; Tecle, H; Thompson, AM; Trachet, E; Winters, RT; Zhu, T1
Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP1
Guo, Y; He, J; Li, Y; Liu, M; Liu, Y; Xiao, J; Yu, W; Zhang, Q1
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Grünwald, V; Hidalgo, M1
Berlin, JD; Lockhart, AC; Lockhart, C1
Albanell, J; Gascón, P1
Bell, DW; Brannigan, BW; Driscoll, DR; Fidias, P; Godin-Heymann, N; Haber, DA; Harris, PL; Isselbacher, KJ; Kwak, EL; Lynch, TJ; McGinnis, JP; Okimoto, RA; Rabindran, SK; Settleman, J; Sharma, SV; Sordella, R; Wissner, A1
Costello, G; Holloway, B; Speake, G1
Fukuoka, M; Hirata, K; Kimura, T; Kudoh, S; Matsui, K; Matsuura, K; Mitsuoka, S; Nakagawa, K; Negoro, S; Yoshimura, N1
Baselga, J1
Breza, N; Keri, G; Orfi, L; Petak, I; Pinter, F; Robert, K; Schwab, R; Varkondi, E1
Pandiella, A; Sánchez-Martín, M1
Antalffy, G; Hegedüs, C; Kéri, G; Német, K; Orfi, L; Ozvegy-Laczka, C; Sarkadi, B; Settleman, J; Szakács, G; Truta-Feles, K; Váradi, A; Várady, G1
Ahn, HJ; Bhatt, L; Kim, YH; Lee, WK; Nam, HW; Yang, Z1

Reviews

5 review(s) available for gefitinib and ekb 569

ArticleYear
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
    Bioorganic & medicinal chemistry, 2019, 02-01, Volume: 27, Issue:3

    Topics: Animals; Antineoplastic Agents; Cell Proliferation; Humans; Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Quinazolines

2019
Developing inhibitors of the epidermal growth factor receptor for cancer treatment.
    Journal of the National Cancer Institute, 2003, Jun-18, Volume: 95, Issue:12

    Topics: Aminoquinolines; Aniline Compounds; Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cetuximab; Clinical Trials as Topic; Drug Design; Drugs, Investigational; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Morpholines; Neoplasms; Organic Chemicals; Panitumumab; Pyrimidines; Pyrroles; Quinazolines; Signal Transduction; Structure-Activity Relationship

2003
The epidermal growth factor receptor as a target for colorectal cancer therapy.
    Seminars in oncology, 2005, Volume: 32, Issue:1

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cell Transformation, Neoplastic; Cetuximab; Colorectal Neoplasms; Disease Progression; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Organic Chemicals; Panitumumab; Prognosis; Pyrimidines; Pyrroles; Quinazolines; Signal Transduction

2005
Small molecules with EGFR-TK inhibitor activity.
    Current drug targets, 2005, Volume: 6, Issue:3

    Topics: Aminoquinolines; Aniline Compounds; Animals; Antineoplastic Agents; Clinical Trials as Topic; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Intracellular Signaling Peptides and Proteins; Mutation; Neoplasms; Organic Chemicals; Quinazolines; Signal Transduction

2005
Recent developments related to the EGFR as a target for cancer chemotherapy.
    Current opinion in pharmacology, 2005, Volume: 5, Issue:4

    Topics: Aminoquinolines; Aniline Compounds; Carcinoma, Non-Small-Cell Lung; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Molecular Structure; Organic Chemicals; Protein Kinase Inhibitors; Quinazolines

2005

Trials

1 trial(s) available for gefitinib and ekb 569

ArticleYear
EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib.
    Lung cancer (Amsterdam, Netherlands), 2006, Volume: 51, Issue:3

    Topics: Administration, Oral; Aminoquinolines; Aniline Compounds; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; Female; Gefitinib; Humans; Japan; Lung Neoplasms; Magnetic Resonance Imaging; Male; Middle Aged; Organic Chemicals; Quinazolines; Tomography, X-Ray Computed; Treatment Outcome

2006

Other Studies

18 other study(ies) available for gefitinib and ekb 569

ArticleYear
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
    Bioorganic & medicinal chemistry letters, 2002, Oct-21, Volume: 12, Issue:20

    Topics: Antineoplastic Agents; Cell Line; Cyclization; Enzyme Inhibitors; ErbB Receptors; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Molecular Conformation; Nitriles; Quinolines; Receptor, ErbB-2

2002
A small molecule-kinase interaction map for clinical kinase inhibitors.
    Nature biotechnology, 2005, Volume: 23, Issue:3

    Topics: Benzamides; Drug Design; Escherichia coli; Escherichia coli Proteins; Imatinib Mesylate; Microchemistry; Pharmaceutical Preparations; Piperazines; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Pyrimidines

2005
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
    Bioorganic & medicinal chemistry, 2007, Jun-01, Volume: 15, Issue:11

    Topics: Adenosine Triphosphate; Binding Sites; Biological Assay; Cells, Cultured; ErbB Receptors; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Structure; Protein Conformation; Protein Kinase Inhibitors; Quinazolines; Vascular Endothelial Growth Factor Receptor-2

2007
A quantitative analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2008, Volume: 26, Issue:1

    Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship

2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2011
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
    Journal of medicinal chemistry, 2013, Sep-12, Volume: 56, Issue:17

    Topics: ErbB Receptors; Models, Molecular; Mutation; Structure-Activity Relationship

2013
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
    Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8

    Topics: Antiviral Agents; Cell Line; Crystallography, X-Ray; Hepacivirus; Hepatitis C; Humans; Intracellular Signaling Peptides and Proteins; Models, Molecular; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyridines; Thiazoles; Virus Internalization

2015
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
    European journal of medicinal chemistry, 2015, Sep-18, Volume: 102

    Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; MCF-7 Cells; Molecular Structure; Protein Kinase Inhibitors; Quinolines; Structure-Activity Relationship

2015
Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.
    ACS chemical biology, 2016, 05-20, Volume: 11, Issue:5

    Topics: Benzocycloheptenes; Cell Line, Tumor; Ferrochelatase; Heme; Humans; Imidazoles; Indoles; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Proteomics; Pyrazines; Pyridines; Quinolines; Sulfonamides; Vemurafenib

2016
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.
    Journal of medicinal chemistry, 2016, 09-08, Volume: 59, Issue:17

    Topics: Administration, Oral; Animals; Antineoplastic Agents; Dogs; ErbB Receptors; Heterografts; Humans; Injections, Intravenous; Macaca fascicularis; Male; Mice, Nude; Morpholines; Neoplasm Transplantation; Phosphorylation; Pyridines; Pyrimidines; Quinazolines; Quinazolinones; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship

2016
The target landscape of clinical kinase drugs.
    Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
    Journal of medicinal chemistry, 2019, 05-09, Volume: 62, Issue:9

    Topics: Aminoquinolines; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Chordoma; Drug Design; ErbB Receptors; HEK293 Cells; Humans; Intracellular Signaling Peptides and Proteins; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Quinazolines

2019
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.
    Proceedings of the National Academy of Sciences of the United States of America, 2005, May-24, Volume: 102, Issue:21

    Topics: Aminoquinolines; Aniline Compounds; Base Sequence; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Drug Resistance; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Immunoblotting; Lung Neoplasms; Molecular Sequence Data; Mutation; Neoplasm Recurrence, Local; Organic Chemicals; Phosphorylation; Quinazolines; Quinolines; Receptor, ErbB-2; Sequence Analysis, DNA; Signal Transduction; Tumor Cells, Cultured

2005
Is there a role for the irreversible epidermal growth factor receptor inhibitor EKB-569 in the treatment of cancer? A mutation-driven question.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2006, May-20, Volume: 24, Issue:15

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antineoplastic Agents; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Mutation; Neoplasms; Organic Chemicals; Protein Kinase Inhibitors; Quinazolines

2006
Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor.
    Journal of receptor and signal transduction research, 2008, Volume: 28, Issue:3

    Topics: Aminoquinolines; Aniline Compounds; Biological Assay; Drug Resistance; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Inhibitory Concentration 50; Morpholines; Mutant Proteins; Protein Kinase Inhibitors; Quinazolines; Substrate Specificity; Tyrphostins

2008
Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.
    International journal of cancer, 2012, Jul-01, Volume: 131, Issue:1

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Morpholines; Protein Kinase Inhibitors; Protein Multimerization; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2012
Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance.
    Biochemical pharmacology, 2012, Aug-01, Volume: 84, Issue:3

    Topics: Aminoquinolines; Aniline Compounds; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Cell Line; Cell Survival; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Humans; Neoplasm Proteins; Piperidines; Protein Binding; Quinazolines; Quinolines

2012
Suppressors for Human Epidermal Growth Factor Receptor 2/4 (HER2/4): A New Family of Anti-Toxoplasmic Agents in ARPE-19 Cells.
    The Korean journal of parasitology, 2017, Volume: 55, Issue:5

    Topics: Afatinib; Aminoquinolines; Aniline Compounds; Animals; Cell Line; Gefitinib; Humans; Mice, Inbred BALB C; Protein Kinase Inhibitors; Quinazolines; Quinazolinones; Quinolines; Receptor, ErbB-2; Toxoplasma; Tyrphostins

2017