Page last updated: 2024-08-18

thiophenes and osi 930

thiophenes has been researched along with osi 930 in 12 studies

Research

Studies (12)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (50.00)29.6817
2010's6 (50.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Castaldo, L; Garton, A; Haack, H; Haley, JD; Hunt, T; Kahler, J; McCormack, S; Nuwaysir, L; Petti, F; Sullivan, L; Thelemann, A; Zeiske, L1
Bockman, J; Rice, MC1
Arnold, LD; Bittner, MA; Briner, P; Brown, EN; Castaldo, L; Castelhano, AL; Chan, A; Cooke, AR; Crew, AP; Emerson, DL; Franklin, M; Franks, A; Garton, AJ; Gibson, NW; Hart, K; Henninger, D; Hidden, C; Kahler, J; Keily, JF; Li, AH; O'Connor, M; Pirrit, C; Richardson, F; Sennello, R; Srebernak, MC; Vulevic, B; Winski, SL; Wynne, GM; Zhang, T1
Johnson, WW; Medower, C; Wen, L1
Epstein, D; Haley, JD; Petti, F; Sujka-Kwok, I; Thomson, S1
Dihel, L; Johnson, WW; Kittleson, C; Mulvihill, K1
Hollenberg, PF; Johnson, WW; Lin, HL; Medower, C; Zhang, H1
Barr, S; Chou, J; Depeille, P; Epstein, DM; Falcon, BL; Fogarty, J; Gokhale, PC; McDonald, DM; Miglarese, M1
Chen, ZS; Korlipara, VL; Kuang, YH; Patel, JP1
Ambudkar, SV; Chen, X; Chen, ZS; Dai, CL; Fu, LW; Korlipara, VL; Kuang, YH; Liao, LQ; Patel, A; Patel, JP; Sodani, K; Tiwari, AK; Wu, CP1
Brock, K; Evans, TR; Gedrich, R; Hopkins, CA; Macpherson, IR; Poondru, S; Simon, GR; Stephens, A; Stewart, K1
Arkenau, HT; Boinpally, R; Brock, K; Camidge, DR; Chick, J; Demetri, G; Desouza, NM; Eckhardt, SG; Gedrich, R; George, S; Gwyther, SJ; Kaye, SB; Lal, R; Leach, MO; Poondru, S; Scurr, M; Serkova, NJ; Spicer, J; Spratlin, JL; Stephens, A; Yap, TA1

Trials

2 trial(s) available for thiophenes and osi 930

ArticleYear
A phase 1 study of OSI-930 in combination with erlotinib in patients with advanced solid tumours.
    European journal of cancer (Oxford, England : 1990), 2013, Volume: 49, Issue:4

    Topics: Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Area Under Curve; Dose-Response Relationship, Drug; ErbB Receptors; Erlotinib Hydrochloride; Female; Humans; Male; Maximum Tolerated Dose; Middle Aged; Neoplasms; Prognosis; Protein Kinase Inhibitors; Quinazolines; Quinolines; Thiophenes; Tissue Distribution

2013
First-in-human phase I trial of two schedules of OSI-930, a novel multikinase inhibitor, incorporating translational proof-of-mechanism studies.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2013, Feb-15, Volume: 19, Issue:4

    Topics: Adult; Aged; Aged, 80 and over; Fatigue; Female; Humans; Male; Maximum Tolerated Dose; Middle Aged; Neoplasms; Positron-Emission Tomography; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinolines; Thiophenes; Vascular Endothelial Growth Factor Receptor-2

2013

Other Studies

10 other study(ies) available for thiophenes and osi 930

ArticleYear
Temporal quantitation of mutant Kit tyrosine kinase signaling attenuated by a novel thiophene kinase inhibitor OSI-930.
    Molecular cancer therapeutics, 2005, Volume: 4, Issue:8

    Topics: Antineoplastic Agents; Humans; Leukemia, Mast-Cell; Mutation; Neoplasm Proteins; Peptides; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-kit; Quinolines; Signal Transduction; Thiophenes; Tissue Array Analysis; Tumor Cells, Cultured

2005
Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit.
    IDrugs : the investigational drugs journal, 2005, Volume: 8, Issue:10

    Topics: Angiogenesis Inhibitors; Benzamides; Chemistry, Pharmaceutical; Clinical Trials as Topic; Cooperative Behavior; Diphenylamine; Drug Industry; Drugs, Investigational; Humans; Lenalidomide; Marketing; Phthalazines; Piperazines; Protein Serine-Threonine Kinases; Pyrazoles; Pyridines; Quinolines; Receptor Protein-Tyrosine Kinases; Receptor, Transforming Growth Factor-beta Type II; Receptors, Transforming Growth Factor beta; Stem Cell Factor; Thalidomide; Thiophenes; Vascular Endothelial Growth Factor A

2005
OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models.
    Cancer research, 2006, Jan-15, Volume: 66, Issue:2

    Topics: Administration, Oral; Animals; Female; Humans; Leukemia, Mast-Cell; Mice; Mice, Nude; Proto-Oncogene Proteins c-kit; Quinolines; Thiophenes; Transplantation, Heterologous; Vascular Endothelial Growth Factor Receptor-2

2006
Cytochrome P450 oxidation of the thiophene-containing anticancer drug 3-[(quinolin-4-ylmethyl)-amino]-thiophene-2-carboxylic acid (4-trifluoromethoxy-phenyl)-amide to an electrophilic intermediate.
    Chemical research in toxicology, 2008, Volume: 21, Issue:8

    Topics: Antineoplastic Agents; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme System; DNA Damage; DNA-Binding Proteins; Glutathione; Half-Life; Humans; Liver; Microsomes, Liver; Oxidation-Reduction; Protein Binding; Quinolines; Recombinant Proteins; Spectrometry, Mass, Electrospray Ionization; Sulfoxides; Tandem Mass Spectrometry; Thiophenes

2008
Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy.
    Clinical & experimental metastasis, 2008, Volume: 25, Issue:8

    Topics: Benzimidazoles; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Chromatography, Liquid; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Humans; Immunoblotting; Lung Neoplasms; Mesoderm; Mitogen-Activated Protein Kinase Kinases; Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-akt; Pyrimidines; Quinazolines; Quinolines; Receptor, ErbB-2; Receptor, ErbB-3; Receptors, Fibroblast Growth Factor; Receptors, Platelet-Derived Growth Factor; Respiratory Mucosa; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Signal Transduction; Spectrometry, Mass, Electrospray Ionization; Thiophenes; Transforming Growth Factor beta; Tumor Cells, Cultured

2008
Oxidative metabolism of the trifluoromethoxy moiety of OSI-930.
    Drug metabolism and drug interactions, 2009, Volume: 24, Issue:2-4

    Topics: Animals; Biotransformation; Chromatography, Liquid; Cytochrome P-450 Enzyme System; Humans; Microsomes, Liver; Oxidation-Reduction; Quinolines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tandem Mass Spectrometry; Thiophenes

2009
Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug.
    Drug metabolism and disposition: the biological fate of chemicals, 2011, Volume: 39, Issue:2

    Topics: Antineoplastic Agents; Binding Sites; Biotransformation; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Cytochromes b5; Dose-Response Relationship, Drug; Escherichia coli; Humans; Molecular Structure; Oxidation-Reduction; Protein Binding; Quinolines; Thiophenes

2011
Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors.
    Cancer research, 2011, Mar-01, Volume: 71, Issue:5

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Humans; Immunohistochemistry; Mechanistic Target of Rapamycin Complex 1; Mice; Mice, Nude; Microscopy, Confocal; Multiprotein Complexes; Neoplasms, Experimental; Neovascularization, Pathologic; Proteins; Quinolines; Sirolimus; Thiophenes; TOR Serine-Threonine Kinases; Transcription Factors; Vascular Endothelial Growth Factor A; Xenograft Model Antitumor Assays

2011
Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930.
    Bioorganic & medicinal chemistry letters, 2011, Nov-01, Volume: 21, Issue:21

    Topics: ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Cell Line; Humans; Inhibitory Concentration 50; Neoplasm Proteins; Proto-Oncogene Proteins c-kit; Quinolines; Thiophenes; Vascular Endothelial Growth Factor Receptor-2

2011
OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance.
    Biochemical pharmacology, 2012, Sep-15, Volume: 84, Issue:6

    Topics: Adenosine Triphosphatases; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Azides; Benzene Derivatives; Biological Transport; Cells, Cultured; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; Mitoxantrone; Neoplasm Proteins; Nitro Compounds; Photoaffinity Labels; Prazosin; Pyridines; Quinolines; Structure-Activity Relationship; Thiophenes; Transfection

2012