Page last updated: 2024-09-05

lapatinib and pf 00299804

lapatinib has been researched along with pf 00299804 in 12 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(pf 00299804)
Trials
(pf 00299804)
Recent Studies (post-2010) (pf 00299804)
1,9193051,44218041172

Protein Interaction Comparison

ProteinTaxonomylapatinib (IC50)pf 00299804 (IC50)
Epidermal growth factor receptorHomo sapiens (human)0.037
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.0392
Tyrosine-protein kinase LckHomo sapiens (human)0.094
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)0.11
Receptor tyrosine-protein kinase erbB-3Homo sapiens (human)0.0006
Mitogen-activated protein kinase kinase kinase 8Homo sapiens (human)3.57
Tyrosine-protein kinase JAK3Homo sapiens (human)3.57
Receptor tyrosine-protein kinase erbB-4Homo sapiens (human)0.0494

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's10 (83.33)24.3611
2020's2 (16.67)2.80

Authors

AuthorsStudies
Abouzid, KAM; Lasheen, DS; Milik, SN; Serya, RAT1
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
Das, D; Hong, J1
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Abd El-Karim, SS; Ahmed, NS; Anwar, MM; El-Hallouty, SM; Srour, AM1
Chen, XB; Wang, S; Wang, SQ; Yu, B; Yuan, XH; Zhao, W1
Anderson, L; Britten, CD; Christensen, JG; Cohen, DJ; Conklin, D; Desai, AJ; Finn, RS; Ginther, C; Kalous, O; O'Brien, NA; Slamon, DJ; Taylor, I1
Mehra, R; Zibelman, M1
Amici, A; Andreani, C; Bartolacci, C; Belletti, B; Elexpuru Zabaleta, M; Galeazzi, R; Gambini, V; Garulli, C; Hysi, A; Iezzi, M; Kalogris, C; Marchini, C; Orlando, F; Pietrella, L; Provinciali, M; Tilio, M; Wang, J1
Abdelhameed, AS; AlRabiah, H; Attwa, MW; Kadi, AA1
D'Abronzo, LS; Drake, CM; Ghosh, PM; Jathal, MK; Mooso, BA; Siddiqui, S; Steele, TM; Whang, YE1

Reviews

5 review(s) available for lapatinib and pf 00299804

ArticleYear
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
    European journal of medicinal chemistry, 2017, Dec-15, Volume: 142

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Resistance, Neoplasm; ErbB Receptors; Gene Amplification; Humans; Models, Molecular; Neoplasms; Point Mutation; Protein Domains; Protein Kinase Inhibitors; Receptor, ErbB-2

2017
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
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
    European journal of medicinal chemistry, 2019, May-15, Volume: 170

    Topics: Animals; Antineoplastic Agents; Chemistry Techniques, Synthetic; Humans; Neoplasms; Protein Kinase Inhibitors; Quinazolines

2019
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
    European journal of medicinal chemistry, 2021, Mar-15, Volume: 214

    Topics: Antineoplastic Agents; Bridged Bicyclo Compounds, Heterocyclic; Humans; Molecular Structure; Neoplasms; Pyrimidines; United States; United States Food and Drug Administration

2021
Overview of Current Treatment Options and Investigational Targeted Therapies for Locally Advanced Squamous Cell Carcinoma of the Head and Neck.
    American journal of clinical oncology, 2016, Volume: 39, Issue:4

    Topics: Afatinib; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Azepines; Carcinoma, Squamous Cell; Cetuximab; Dasatinib; ErbB Receptors; Erlotinib Hydrochloride; Head and Neck Neoplasms; Humans; Lapatinib; Molecular Targeted Therapy; Panitumumab; Protein Kinase Inhibitors; Pyrimidines; Quinazolines; Quinazolinones; Signal Transduction; Sirolimus

2016

Other Studies

7 other study(ies) available for lapatinib and pf 00299804

ArticleYear
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
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
    Bioorganic & medicinal chemistry, 2020, 09-15, Volume: 28, Issue:18

    Topics: Antineoplastic Agents; Apoptosis; Benzimidazoles; Breast Neoplasms; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Erlotinib Hydrochloride; Female; Humans; MCF-7 Cells; Molecular Docking Simulation; Protein Kinase Inhibitors; Quantitative Structure-Activity Relationship; Thiazoles

2020
Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib.
    Molecular cancer therapeutics, 2012, Volume: 11, Issue:9

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Hormonal; Apoptosis; Breast Neoplasms; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; Female; Gene Amplification; Humans; Inhibitory Concentration 50; Lapatinib; Neoplasms, Hormone-Dependent; Phosphorylation; Protein Processing, Post-Translational; Quinazolines; Quinazolinones; Receptor, ErbB-2; Receptors, Estrogen; Signal Transduction; Trastuzumab

2012
Irreversible inhibition of Δ16HER2 is necessary to suppress Δ16HER2-positive breast carcinomas resistant to Lapatinib.
    Cancer letters, 2016, 10-10, Volume: 381, Issue:1

    Topics: Alternative Splicing; Animals; Benzodioxoles; Breast Neoplasms; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Female; Genetic Predisposition to Disease; Humans; Inhibitory Concentration 50; Lapatinib; Mammary Neoplasms, Experimental; Mice, Transgenic; Phenotype; Protein Isoforms; Protein Kinase Inhibitors; Quinazolines; Quinazolinones; Receptor, ErbB-2; Signal Transduction; Time Factors

2016
Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability.
    PloS one, 2019, Volume: 14, Issue:4

    Topics: Animals; Chromatography, High Pressure Liquid; Lapatinib; Limit of Detection; Microsomes, Liver; Quinazolinones; Rats; Tandem Mass Spectrometry

2019
Dacomitinib, but not lapatinib, suppressed progression in castration-resistant prostate cancer models by preventing HER2 increase.
    British journal of cancer, 2019, Volume: 121, Issue:3

    Topics: Animals; Cell Line, Tumor; Disease Models, Animal; ErbB Receptors; Humans; Lapatinib; Male; Mice; Mice, Inbred BALB C; Prostatic Neoplasms, Castration-Resistant; Protein Multimerization; Quinazolinones; Receptor, ErbB-2

2019