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imatinib and Gastrointestinal Stromal Neoplasm

imatinib has been researched along with Gastrointestinal Stromal Neoplasm in 8 studies

Research Excerpts

ExcerptRelevanceReference
"9%, 1-resistant GISTs) at a dosage of 100 mg/kg/day without exhibiting apparent toxicity."5.46Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). ( Li, J; Li, X; Lu, Y; Mao, F; Wang, M; Xu, Q; Zheng, X; Zhu, J, 2017)
" Here we describe the identification of potent pan-KIT mutant kinase inhibitors that can be dosed without being limited by the tolerability issues seen with multitargeted agents."1.48Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. ( Anjum, R; Barry, E; Bhavsar, D; Boyd, S; Brown, C; Campbell, A; Goldberg, K; Grondine, M; Guichard, S; Hardy, CJ; Hunt, T; Jones, RDO; Kettle, JG; Li, X; Moleva, O; Ogg, D; Overman, RC; Packer, MJ; Pearson, S; Schimpl, M; Shao, W; Smith, A; Smith, JM; Stead, D; Stokes, S; Tucker, M; Ye, Y, 2018)
"9%, 1-resistant GISTs) at a dosage of 100 mg/kg/day without exhibiting apparent toxicity."1.46Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). ( Li, J; Li, X; Lu, Y; Mao, F; Wang, M; Xu, Q; Zheng, X; Zhu, J, 2017)
" In addition, 13 possessed acceptable bioavailability (36%) and effectively suppressed the tumor growth in GIST-T1 cell inoculated xenograft model without apparent toxicity."1.43Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). ( Chen, C; Hu, Z; Liu, F; Liu, J; Liu, Q; Liu, X; Qi, S; Qi, Z; Wang, A; Wang, B; Wang, L; Wang, Q; Wang, W; Wang, Y; Zhang, S; Zhao, Z; Zou, F, 2016)
" In the BaF3-TEL-cKIT-T670I isogenic cell inoculated xenograft mouse model, 35 exhibited dose dependent tumor growth suppression efficacy and 100 mg/kg dosage provided 47."1.43Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina ( Bai, M; Chen, C; Hu, C; Hu, Z; Li, B; Liu, F; Liu, J; Liu, Q; Liu, X; Qi, Z; Ren, T; Wang, A; Wang, B; Wang, L; Wang, W; Wu, H; Wu, J; Ye, L; Yu, K; Zhang, S; Zou, F, 2016)
"Most of human gastrointestinal stromal tumors (GIST) are driven by activating mutations in the proto-oncogene KIT, a tyrosine kinase receptor."1.35Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. ( Beltran, M; Cuenca, F; Fletcher, JA; Galesa, K; Gunaratnam, M; Haider, SM; Neidle, S; Reszka, AP; Swank, S, 2009)

Research

Studies (8)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (12.50)29.6817
2010's7 (87.50)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Gunaratnam, M1
Swank, S1
Haider, SM1
Galesa, K1
Reszka, AP1
Beltran, M1
Cuenca, F1
Fletcher, JA1
Neidle, S1
Wang, Q1
Liu, F2
Wang, B3
Zou, F3
Chen, C3
Liu, X3
Wang, A3
Qi, S1
Wang, W5
Qi, Z3
Zhao, Z1
Hu, Z3
Wang, L3
Zhang, S3
Wang, Y1
Liu, J4
Liu, Q4
Li, B1
Yu, K2
Wu, H1
Hu, C2
Wu, J1
Ye, L1
Ren, T2
Bai, M2
Lu, Y1
Mao, F1
Li, X2
Zheng, X1
Wang, M1
Xu, Q1
Zhu, J1
Li, J1
Kettle, JG1
Anjum, R1
Barry, E1
Bhavsar, D1
Brown, C1
Boyd, S1
Campbell, A1
Goldberg, K1
Grondine, M1
Guichard, S1
Hardy, CJ1
Hunt, T1
Jones, RDO1
Moleva, O1
Ogg, D1
Overman, RC1
Packer, MJ1
Pearson, S1
Schimpl, M1
Shao, W1
Smith, A1
Smith, JM1
Stead, D1
Stokes, S1
Tucker, M1
Ye, Y1
Wu, TS2
Lin, WH2
Tsai, HJ2
Hsueh, CC2
Hsu, T2
Wang, PC2
Lin, HY2
Peng, YH2
Lu, CT2
Lee, LC1
Tu, CH1
Kung, FC2
Shiao, HY2
Yeh, TK2
Song, JS2
Chang, JY1
Su, YC2
Chen, LT2
Chen, CT2
Jiaang, WT2
Wu, SY2
Wang, J1
Ge, J1
Jiang, Z1
Kuo, CC1
Chen, CP1
Weng, YL1
Wu, MH1
Huang, KW1
Chou, LH1
Yen, KJ1
Kuo, PC1
Huang, CL1
Shih, C1

Other Studies

8 other studies available for imatinib and Gastrointestinal Stromal Neoplasm

ArticleYear
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
    Journal of medicinal chemistry, 2009, Jun-25, Volume: 52, Issue:12

    Topics: Base Sequence; Cell Line, Tumor; Cell Proliferation; Computer Simulation; Dose-Response Relationship

2009
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
    Journal of medicinal chemistry, 2016, 04-28, Volume: 59, Issue:8

    Topics: Administration, Oral; Animals; Area Under Curve; Benzamides; Cell Line, Tumor; Drug Discovery; Gastr

2016
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina
    Journal of medicinal chemistry, 2016, 09-22, Volume: 59, Issue:18

    Topics: Amides; Animals; Cell Line, Tumor; Female; Gastrointestinal Neoplasms; Gastrointestinal Stromal Tumo

2016
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).
    Journal of medicinal chemistry, 2017, 06-22, Volume: 60, Issue:12

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Chemistry Techniques, Synthetic; Drug Resistance,

2017
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
    Journal of medicinal chemistry, 2018, 10-11, Volume: 61, Issue:19

    Topics: Drug Discovery; Gastrointestinal Neoplasms; Gastrointestinal Stromal Tumors; Humans; Models, Molecul

2018
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.
    Journal of medicinal chemistry, 2019, 04-25, Volume: 62, Issue:8

    Topics: Animals; Binding Sites; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Drug Evaluatio

2019
Discovery of ( E)- N
    Journal of medicinal chemistry, 2019, 05-23, Volume: 62, Issue:10

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug R

2019
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.
    Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Female; fms-Like Tyrosine Kinase 3; G

2019