Page last updated: 2024-09-03

gefitinib and pi103

gefitinib has been researched along with pi103 in 11 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(pi103)
Trials
(pi103)
Recent Studies (post-2010) (pi103)
5,2315662,9191810139

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)pi103 (IC50)
Chain A, PHOSPHOTIDYLINOSITOL 3 KINASE 59FDrosophila melanogaster (fruit fly)2.3
Chain A, PHOSPHOTIDYLINOSITOL 3 KINASE 59FDrosophila melanogaster (fruit fly)2.3
Chain A, PHOSPHOTIDYLINOSITOL 3 KINASE 59FDrosophila melanogaster (fruit fly)2.3
Chain A, PHOSPHOTIDYLINOSITOL 3 KINASE 59FDrosophila melanogaster (fruit fly)2.3
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)0.0155
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alphaHomo sapiens (human)1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit betaHomo sapiens (human)0.0585
Cytochrome P450 1A2Homo sapiens (human)0.012
Cytochrome P450 3A4Homo sapiens (human)0.0111
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)0.011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)0.011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)0.011
Phosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)0.0114
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)0.2038
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)0.0346
Serine/threonine-protein kinase mTORHomo sapiens (human)0.4746
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)0.069
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)0.0215
Rapamycin-insensitive companion of mTORHomo sapiens (human)0.083
Regulatory-associated protein of mTORHomo sapiens (human)0.02
Target of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)0.083
Target of rapamycin complex subunit LST8Homo sapiens (human)0.041

Research

Studies (11)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (36.36)29.6817
2010's7 (63.64)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Bullock, AN; Fedorov, O; Knapp, S; Marsden, B; Müller, S; Pogacic, V; Rellos, P; Schwaller, J; Sundström, M1
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
Aizenstein, B; Apsel, B; Blair, JA; Feldman, ME; Gonzalez, B; Hoffman, R; Knight, ZA; Nazif, TM; Shokat, KM; Williams, RL1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Russu, WA; Shallal, HM1
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
Li, D; Shen, QJ; Wang, F; Xing, WH; Xu, J; Zhang, LN; Zhang, XH; Zhuo, RJ; Zou, ZQ1
Dive, C; Harrison, LR; Mironov, A; Moreira-Leite, FF; Roberts, RA1
Donev, IS; Li, Q; Matsumoto, K; Nishioka, Y; Sone, S; Takeuchi, S; Wang, W; Yamada, T; Yamori, T; Yano, S1
Bae, I; Hong, W; Kang, HJ; Kim, HJ; Seong, YS; Wang, A; Yi, YW; Zhao, W1

Other Studies

11 other study(ies) available for gefitinib and pi103

ArticleYear
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
    Proceedings of the National Academy of Sciences of the United States of America, 2007, Dec-18, Volume: 104, Issue:51

    Topics: Amino Acid Sequence; Binding Sites; Clinical Trials as Topic; Drug Evaluation, Preclinical; Enzyme Stability; Humans; Molecular Sequence Data; Phylogeny; Protein Array Analysis; Protein Conformation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases

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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
    Nature chemical biology, 2008, Volume: 4, Issue:11

    Topics: Amino Acid Sequence; Antineoplastic Agents; Apoptosis; Blotting, Western; Catalytic Domain; Cell Proliferation; Cells, Cultured; Crystallography, X-Ray; Drug Delivery Systems; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Fusion Proteins, bcr-abl; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Molecular Structure; Phosphoinositide-3 Kinase Inhibitors; Protein Kinases; Protein Subunits; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Sequence Alignment; Signal Transduction; TOR Serine-Threonine Kinases

2008
Navigating the kinome.
    Nature chemical biology, 2011, Volume: 7, Issue:4

    Topics: Drug Design; Pharmacogenetics; Protein Kinases; Proteome; Systems Biology

2011
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
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
A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells.
    International journal of molecular medicine, 2009, Volume: 24, Issue:1

    Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Class I Phosphatidylinositol 3-Kinases; Drug Resistance, Neoplasm; Furans; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Lung Neoplasms; Mutation; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Protein Kinases; Pyridines; Pyrimidines; Quinazolines; TOR Serine-Threonine Kinases; Tumor Suppressor Proteins

2009
Inducible EGFR T790M-mediated gefitinib resistance in non-small cell lung cancer cells does not modulate sensitivity to PI103 provoked autophagy.
    Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, 2010, Volume: 5, Issue:6

    Topics: Antineoplastic Agents; Autophagy; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Extracellular Signal-Regulated MAP Kinases; Furans; Gefitinib; Humans; Intracellular Signaling Peptides and Proteins; Lung Neoplasms; Mutation; Phosphoinositide-3 Kinase Inhibitors; Phosphorylation; Protein Serine-Threonine Kinases; Pyridines; Pyrimidines; Quinazolines; TOR Serine-Threonine Kinases

2010
Transient PI3K inhibition induces apoptosis and overcomes HGF-mediated resistance to EGFR-TKIs in EGFR mutant lung cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2011, Apr-15, Volume: 17, Issue:8

    Topics: Animals; Apoptosis; Blotting, Western; Cell Line; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Female; Furans; Gefitinib; Hepatocyte Growth Factor; Humans; Lung Neoplasms; Mice; Mice, SCID; Mutation; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Pyridines; Pyrimidines; Quinazolines; Signal Transduction; Xenograft Model Antitumor Assays

2011
Inhibition of the PI3K/AKT pathway potentiates cytotoxicity of EGFR kinase inhibitors in triple-negative breast cancer cells.
    Journal of cellular and molecular medicine, 2013, Volume: 17, Issue:5

    Topics: Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Caspases; Cell Death; Cell Line, Tumor; Drug Synergism; ErbB Receptors; Extracellular Signal-Regulated MAP Kinases; Female; Furans; Gefitinib; Humans; Inhibitory Concentration 50; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyridines; Pyrimidines; Quinazolines; Signal Transduction

2013