Page last updated: 2024-09-03

gefitinib and hki 272

gefitinib has been researched along with hki 272 in 24 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(hki 272)
Trials
(hki 272)
Recent Studies (post-2010) (hki 272)
5,2315662,91928342248

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)hki 272 (IC50)
Epidermal growth factor receptorHomo sapiens (human)0.0416
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.0298
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.8582
Serine/threonine-protein kinase Nek2Homo sapiens (human)0.274

Research

Studies (24)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (29.17)29.6817
2010's16 (66.67)24.3611
2020's1 (4.17)2.80

Authors

AuthorsStudies
Cheung, K; Dushin, RG; Floyd, MB; Fraser, HL; Ingalls, CL; Loganzo, F; Nittoli, T; Ravi, MR; Tan, X; Wissner, A1
Alberti, JG; Alligood, KJ; Caferro, TR; Chamberlain, SD; Dickerson, SH; Dickson, HD; Emerson, HK; Gerding, RM; Griffin, RJ; Hubbard, RD; Keith, BR; Mullin, RJ; Petrov, KG; Reno, MJ; Rheault, TR; Rusnak, DW; Sammond, DM; Smith, SC; Stevens, KL; Uehling, DE; Waterson, AG; Wood, ER1
Bikker, JA; Brooijmans, N; Mansour, TS; Wissner, A1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
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
Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ1
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
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
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Basetti, V; Keesara, M; Maiti, P; Mansour, TS; Moghudula, AG; Pallepati, RR; Potluri, V1
Bauer, S; Baumann, M; Becker, C; Grabe, T; Hardick, J; Hodson, L; Jeyakumar, K; Ketzer, J; Keul, M; Kirschner, T; Klövekorn, P; Lategahn, J; Müller, MP; Niggenaber, J; Rauh, D; Terheyden, S; Tumbrink, HL; Unger, A; van Otterlo, WAL; Weisner, J1
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
Al-Hashem, R; Bronson, RT; Discafani, CM; Eck, M; Glatt, KA; Horner, JW; Ji, H; Jung, BL; Li, D; Maher, E; McNamara, K; Meyerson, M; Mitchell, A; Protopopov, A; Rabindran, SK; Sasaki, H; Shapiro, GI; Shimamura, T; Sun, Y; Thomas, RK; Wong, KK; Xia, H; Yuza, Y; Zhao, X1
Brannigan, BW; Godin-Heymann, N; Haber, DA; Lamb, J; Maheswaran, S; McDermott, U; Settleman, J; Ulkus, L1
Riely, GJ1
Pandiella, A; Sánchez-Martín, M1
Gong, Y; Pao, W1
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
Dziadziuszko, R; Jassem, J1
Eisenstein, M1
Kim, S; Lee, J; Lee, JE; Nam, SJ; Oh, SJ1
Ahn, HJ; Bhatt, L; Kim, YH; Lee, WK; Nam, HW; Yang, Z1

Reviews

1 review(s) available for gefitinib and hki 272

ArticleYear
Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
    Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, 2008, Volume: 3, Issue:6 Suppl 2

    Topics: Carcinoma, Non-Small-Cell Lung; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Drug Resistance, Neoplasm; Drugs, Investigational; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lung Neoplasms; Male; Prognosis; Quinazolines; Quinolines; Risk Assessment; Survival Analysis; Treatment Outcome

2008

Other Studies

23 other study(ies) available for gefitinib and hki 272

ArticleYear
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
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
    Bioorganic & medicinal chemistry letters, 2009, Jan-01, Volume: 19, Issue:1

    Topics: Administration, Oral; Animals; Antineoplastic Agents; ErbB Receptors; Mice; Pharmacokinetics; Pyrimidines; Pyrrolidines; Receptor, ErbB-2; Structure-Activity Relationship

2009
Kinase domain mutations in cancer: implications for small molecule drug design strategies.
    Journal of medicinal chemistry, 2009, Mar-26, Volume: 52, Issue:6

    Topics: Amino Acid Sequence; Antineoplastic Agents; Drug Design; Enzyme Inhibitors; Humans; Molecular Sequence Data; Mutation; Neoplasms; Phosphotransferases; Protein Conformation

2009
Comprehensive analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2011, Oct-30, Volume: 29, Issue:11

    Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity

2011
Identification of potent Yes1 kinase inhibitors using a library screening approach.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship

2013
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
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2013, Volume: 136, Issue:1

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests

2013
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
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
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12

    Topics: Exons; Humans; Mutation; Protein Kinase Inhibitors; Thioctic Acid

2019
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
    Journal of medicinal chemistry, 2020, 10-22, Volume: 63, Issue:20

    Topics: Dose-Response Relationship, Drug; Drug Design; Drug Evaluation, Preclinical; Humans; Kinetics; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor, ErbB-2; Structure-Activity Relationship; Tumor Cells, Cultured

2020
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
Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity to tyrosine kinase inhibitors.
    Proceedings of the National Academy of Sciences of the United States of America, 2006, May-16, Volume: 103, Issue:20

    Topics: Animals; Antineoplastic Agents; Cell Line; Cyclin-Dependent Kinase Inhibitor p16; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Mice; Mice, Knockout; Mutation; Protein Isoforms; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Quinolines; Tumor Suppressor Protein p14ARF

2006
The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor.
    Molecular cancer therapeutics, 2008, Volume: 7, Issue:4

    Topics: Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Cells, Cultured; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Immunoblotting; Lung Neoplasms; Mice; Mutation; Phosphorylation; Protein Kinase Inhibitors; Quinazolines; Quinolines

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
EGFR mutant lung cancer.
    Current topics in microbiology and immunology, 2012, Volume: 355

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Clinical Trials as Topic; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; HSP90 Heat-Shock Proteins; Humans; Molecular Targeted Therapy; Mutation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Quinazolines; Quinolines

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
Epidermal growth factor receptor (EGFR) inhibitors and derived treatments.
    Annals of oncology : official journal of the European Society for Medical Oncology, 2012, Volume: 23 Suppl 10

    Topics: Afatinib; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Biomarkers, Pharmacological; Carcinoma, Non-Small-Cell Lung; Cetuximab; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Neoplasm Staging; Prognosis; Quinazolines; Quinolines; Translational Research, Biomedical; Treatment Outcome

2012
Clinical trials: More trials, fewer tribulations.
    Nature, 2014, May-29, Volume: 509, Issue:7502

    Topics: Antineoplastic Combined Chemotherapy Protocols; Biomarkers, Tumor; Breast Neoplasms; Clinical Trials as Topic; Crizotinib; DNA Mutational Analysis; Drug Approval; Drug Resistance, Neoplasm; Female; Gefitinib; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Humans; Neoplasms; Patient Selection; Proto-Oncogene Proteins B-raf; Pyrazoles; Pyridines; Quinazolines; Quinolines; Sample Size

2014
Differential effect of EGFR inhibitors on tamoxifen-resistant breast cancer cells.
    Oncology reports, 2015, Volume: 34, Issue:3

    Topics: Apoptosis; Breast Neoplasms; Cell Proliferation; Cell Survival; Disease-Free Survival; Drug Resistance, Neoplasm; ErbB Receptors; Estrogen Receptor alpha; Female; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; MCF-7 Cells; Poly (ADP-Ribose) Polymerase-1; Poly(ADP-ribose) Polymerases; Quinazolines; Quinolines; Receptor, ErbB-2; Tamoxifen

2015
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