Page last updated: 2024-09-03

gefitinib and plx4032

gefitinib has been researched along with plx4032 in 12 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(plx4032)
Trials
(plx4032)
Recent Studies (post-2010) (plx4032)
5,2315662,9191,6571031,587

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)plx4032 (IC50)
Chain A, AKAP9-BRAF fusion proteinHomo sapiens (human)0.031
RAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)0.182
Serine/threonine-protein kinase A-RafHomo sapiens (human)0.521
Serine/threonine-protein kinase B-rafHomo sapiens (human)0.0897
Serine/threonine-protein kinase B-raf Mus musculus (house mouse)0.03
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.36
Dual specificity mitogen-activated protein kinase kinase 2Homo sapiens (human)1.5
Dual specificity mitogen-activated protein kinase kinase 1Homo sapiens (human)1.5
Mitogen-activated protein kinase kinase kinase 20Homo sapiens (human)0.0272

Research

Studies (12)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (75.00)24.3611
2020's3 (25.00)2.80

Authors

AuthorsStudies
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Chang, Y; Cheng, H; Ding, K; Lu, J; Lu, X; Luo, J; Ren, X; Tu, Z; Zhang, L; Zhang, Q1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
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
Guo, Y; He, J; Li, Y; Liu, M; Liu, Y; Xiao, J; Yu, W; Zhang, Q1
Alsaghir, FM; El-Gamal, MI; Sbenati, RM; Semreen, AM; Semreen, MH; Shehata, MK1
Bardelli, A; Beijersbergen, RL; Bernards, R; Di Nicolantonio, F; Huang, S; Prahallad, A; Salazar, R; Sun, C; Zecchin, D1
Nishio, K; Togashi, Y1
Boespflug, A; Kaya, A; Kaya, G; Saurat, JH; Saxer-Sekulic, N; Sorg, O; Thomas, L1
Beloueche-Babari, M; Delgado-Goñi, T; Galobart, TC; Leach, MO; Normantaite, D; Wantuch, S; Whittaker, SR1
Flaherty, K; Guhan, S; Ji, Z; Kumar, R; Njauw, CN; Rajadurai, A; Reddy, B; Tsao, H1

Reviews

3 review(s) available for gefitinib and plx4032

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
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.
    Bioorganic & medicinal chemistry, 2021, 01-01, Volume: 29

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Imidazoles; Models, Molecular; Protein Binding; Protein Kinase Inhibitors; Ribosomal Protein S6 Kinases, 90-kDa; Signal Transduction; Structure-Activity Relationship; Thiazoles; Tubulin

2021
[Kinase inhibitors and their resistance].
    Nihon rinsho. Japanese journal of clinical medicine, 2015, Volume: 73, Issue:8

    Topics: Antibodies, Monoclonal, Humanized; Benzamides; Biomarkers, Tumor; Crizotinib; Drug Discovery; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Humans; Imatinib Mesylate; Indoles; Molecular Targeted Therapy; Neoplasms; Niacinamide; Phenylurea Compounds; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrazoles; Pyridines; Pyrimidines; Quinazolines; Signal Transduction; Sorafenib; Sulfonamides; Trastuzumab; Vemurafenib

2015

Other Studies

9 other study(ies) available for gefitinib and plx4032

ArticleYear
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
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.
    Journal of medicinal chemistry, 2014, Mar-27, Volume: 57, Issue:6

    Topics: Blotting, Western; Cell Line, Tumor; Cell Proliferation; Colorectal Neoplasms; Drug Evaluation, Preclinical; Drug Resistance, Neoplasm; ErbB Receptors; Genes, erbB-1; Humans; Indicators and Reagents; Indoles; Melanoma; Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Structure-Activity Relationship; Sulfonamides; Vemurafenib

2014
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
    Journal of medicinal chemistry, 2014, Oct-09, Volume: 57, Issue:19

    Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship

2014
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
Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR.
    Nature, 2012, Jan-26, Volume: 483, Issue:7387

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Cetuximab; Colorectal Neoplasms; Drug Resistance, Neoplasm; Drug Synergism; Enzyme Activation; ErbB Receptors; Erlotinib Hydrochloride; Feedback, Physiological; Female; Gefitinib; HEK293 Cells; Humans; Indoles; Melanoma; Mice; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Quinazolines; RNA Interference; Sulfonamides; Vemurafenib; Xenograft Model Antitumor Assays

2012
RASopathic comedone-like or cystic lesions induced by vemurafenib: a model of skin lesions similar but not identical to those induced by dioxins MADISH.
    Journal of the European Academy of Dermatology and Venereology : JEADV, 2018, Volume: 32, Issue:8

    Topics: Antineoplastic Agents; Chloracne; Cytochrome P-450 CYP1A1; Dioxins; Drug Eruptions; Enzyme Activation; Epidermal Cyst; Erlotinib Hydrochloride; Female; Gefitinib; Hep G2 Cells; Humans; Male; Melanoma; Protein Kinase Inhibitors; Skin Neoplasms; Vemurafenib

2018
Increased inflammatory lipid metabolism and anaplerotic mitochondrial activation follow acquired resistance to vemurafenib in BRAF-mutant melanoma cells.
    British journal of cancer, 2020, Volume: 122, Issue:1

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Survival; Dinoprostone; Drug Resistance, Neoplasm; Gefitinib; Gene Expression Regulation, Neoplastic; Humans; Melanoma; Mitochondria; Mutation; Prostaglandin-E Synthases; Proto-Oncogene Proteins B-raf; Pyruvate Carboxylase; Signal Transduction; Skin Neoplasms; Vemurafenib

2020
Loss of ACK1 Upregulates EGFR and Mediates Resistance to BRAF Inhibition.
    The Journal of investigative dermatology, 2021, Volume: 141, Issue:5

    Topics: Animals; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; HEK293 Cells; Humans; Melanoma; Mice; Protein-Tyrosine Kinases; Proto-Oncogene Proteins B-raf; Signal Transduction; Up-Regulation; Vemurafenib

2021