Inhibition of Tumor Cell Growth, Invasion, and Metastasis by EXEL-2880 (XL880, GSK1363089), a Novel Inhibitor of HGF and VEGF Receptor Tyrosine Kinases

The biology of VEGF and its receptors

Ferrara, N., Gerber, H.-P., & LeCouter, J. (2003) · Nature Medicine · doi:10.1038/nm0603-669 · Cited by 9,591

MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling

Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496

Met, metastasis, motility and more

Birchmeier, C., Birchmeier, W., Gherardi, E., & Woude, G. F. V. (2003) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm1261 · Cited by 2,652

MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib

Bean, J., Brennan, C., Shih, J.-Y., Riely, G., Viale, A., Wang, L., Chitale, D., Motoi, N., Szoke, J., Broderick, S., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0710370104 · Cited by 1,598

Germline and somatic mutations in the tyrosine kinase domain of the MET proto-oncogene in papillary renal carcinomas

Schmidt, L. S., Duh, F.-M. C., Chen, F., Kishida, T., Glenn, G. M., Choyke, P. L., Scherer, S. W., Zhuang, Z., Lubensky, I. A., Dean, M. C., et al. (1997) · Nature Genetics · doi:10.1038/ng0597-68 · Cited by 1,517

Active and Inactive Protein Kinases: Structural Basis for Regulation

Johnson, L. N., Noble, M. E. M., & Owen, D. J. (1996) · Cell · doi:10.1016/s0092-8674(00)81092-2 · Cited by 1,396

Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

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Hypoxia promotes invasive growth by transcriptional activation of the met protooncogene

Pennacchietti, S., Michieli, P., Galluzzo, M., Mazzone, M., Giordano, S., & Comoglio, P. M. (2003) · Cancer Cell · doi:10.1016/s1535-6108(03)00085-0 · Cited by 1,311

Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

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Drug development of MET inhibitors: targeting oncogene addiction and expedience

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LC–MS/MS assay for the quantification of foretinib in rat plasma and its application to preclinical pharmacokinetic study

Guo, N., Zhang, A., Zhuang, H., & Zhang, C. (2020) · Biomedical Chromatography · doi:10.1002/bmc.4862 · Cited by 2

PTSA-induced synthesis, in silico and nano study of novel ethylquinolin–thiazolo–triazole in cervical cancer

Sonker, P., Tamang, R., Mehata, A. K., Nidhar, M., Sharma, V. P., Kumar, V., Muthu, M. S., Koch, B., & Tewari, A. K. (2024) · Future Medicinal Chemistry · doi:10.4155/fmc-2023-0344 · Cited by 1

Foretinib Alleviates Osteoblast Senescence and Protects Against Bone Loss in Ovariectomized Mice by Promoting Osteoblast Differentiation

Oh, J., Lee, J., Kim, E.-C., Kim, J.-R., Ha, H., Kim, T., Lee, K., & Jeong, D. (2025) · Cells · doi:10.3390/cells14241945 · Cited by 1

Overcoming the sorafenib resistance mechanism in FLT3-mutated acute myeloid leukemia: molecular basis and new targets

Peng, H., Li, M., Peng, Y. Y., Li, X. L., Yang, J., Sun, Q. G., & Song, K. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2025.1713174 · Cited by 1

Curation of the Fasciola hepatica kinome as a resource for drug target discovery

Ajmera, S., Puckelwaldt, O., Stroehlein, A. J., & Haeberlein, S. (2026) · BMC Genomics · doi:10.1186/s12864-025-12513-w · Cited by 1

Cyclopropyl as a versatile tool in the development of kinase-targeted therapeutics

Liu, W., Huang, Y., Hao, W., Rong, Z., Liu, X., Zhou, Y., Song, S., & Pang, X. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118761 · Cited by 1

A Structural Perspective on Non-covalent Targeting of Conserved Polar Residues in Protein Kinases

Nasief, N. N., Patel, K. B., Ogboo, B. C., & Heppner, D. E. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00330 · Cited by 1

Impact of Tumor Hypoxia, Src, and Met Signaling in the Dissemination of Tumor Cells

Dai, Y., Shi, W.-Y., Molnar, N., & Siemann, D. (2011) · Springer eBooks · doi:10.1007/978-94-007-2558-4_7 · Cited by 2

Design, Synthesis and Biological Evaluation of Novel 4-phenoxypyridine Derivatives Containing Semicarbazones Moiety as Potential c-Met Kinase Inhibitors

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Simulation-Based Interpretation of Therapeutically Monitored Cabozantinib Plasma Concentration in Advanced Adrenocortical Carcinoma with Hemodialysis

Zimmermann, S., Kurlbaum, M., Mayer, S., Faßnacht, M., Kroiß, M., & Scherf‐Clavel, O. (2021) · Therapeutic Drug Monitoring · doi:10.1097/ftd.0000000000000905 · Cited by 1

Design, Synthesis, and Evaluation of New Mesenchymal–Epithelial Transition Factor (c-Met) Kinase Inhibitors with Dual Chiral Centers

Yao, H., Ren, Y., Yan, J., Liu, J., Hu, J., Yan, M., & Li, X. (2022) · Molecules · doi:10.3390/molecules27175359 · Cited by 1

MET Inhibitors for Papillary Renal Cell Carcinoma

Brundage, J., Sahu, K. K., & Maughan, B. L. (2023) · Kidney Cancer · doi:10.3233/kca-230005 · Cited by 1

Anoikis Resistance in Melanoma

Simmons, J. L., Ng, M. F., Neuendorf, H. M., & Boyle, G. M. (2021) · Springer eBooks · doi:10.1007/978-3-030-73856-3_7 · Cited by 1

Structural and binding studies of human CAMKK2 kinase domain bound to small molecule ligandsPreprint

Profeta, G. S., dos Reis, C. V., Godoi, P. H., Fala, A. M., Sartori, R., Salmazo, A. P. T., Ramos, P. Z., Massirer, K. B., Elkins, J. M., Drewry, D. H., et al. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/538157 · Cited by 1

Hypoxia-induced metastasis : the role of the unfolded protein response

Mujčić, H. (2013) · Research Publications (Maastricht University) · doi:10.26481/dis.20130912hm · Cited by 1

Phase I/II Trial of Cabozantinib Plus Durvalumab in Advanced Gastroesophageal Cancer and Other Gastrointestinal Malignancies (CAMILLA): Phase Ib Safety and Efficacy ResultsPreprint

Saeed, A., Park, R., Dai, J., Al-Rajabi, R., Kasi, A., Baranda, J. C., Williamson, S. K., Saeed, A., Ripp, J., Collins, Z. S., et al. (2022) · SSRN Electronic Journal · doi:10.2139/ssrn.4195069 · Cited by 1

Targeting angiogenesis in non-small-cell lung cancer: a focus on current approaches and future developments

Arango, B. A., Aguirre, L. E. E., Perez, C. A., Velez, M., Santos, E. S., & Raez, L. E. (2013) · Clinical Practice · doi:10.2217/cpr.13.27

Synthesis of tert-butyl 4-((2-methoxy-4-(methoxycarbonyl) phenoxy) methyl) piperidine-1-carboxylate

Wang, M., Wang, W., Tang, Q., & Xu, S. (2015) · International Workshop on Materials Engineering and Computer Sciences (IWMECS) · doi:10.2991/iwmecs-15.2015.46

Study of Molecular Mechanisms of Sensitivity and Resistance to EGFR-Targeted Therapy in Lung Cancer

Zhang, Z. (2010) · OhioLink ETD Center (Ohio Library and Information Network)

Forthcoming Drugs for Metastatic Renal Cell Carcinoma Therapy

Ito, K. (2017) · Springer eBooks · doi:10.1007/978-4-431-55531-5_14

Targeted Therapies in Kidney Cancer

Sánchez-Gastaldo, A., del Alba, A. G., & Durán, I. (2015) · Current clinical pathology · doi:10.1007/978-1-4939-2047-1_15

Identification des voies de signalisations essentielles à la progression tumorale dans les sarcomes : un modèle pour les interactions cellules tumorales et stroma

Blay, J. (2015) · Bulletin de l Académie Nationale de Médecine · doi:10.1016/s0001-4079(19)31004-0

MET as a Therapeutic Target: Have Clinical Outcomes Been “MET” in Lung Cancer?

Nam, A., & Salgia, R. (2019) · Current cancer research · doi:10.1007/978-3-030-17832-1_5

Variant Renal Cell Carcinoma Histologies: Therapeutic Considerations

Geynisman, D. M., & Stadler, W. M. (2011) · Springer eBooks · doi:10.1007/978-3-642-21858-3_17

Design, Molecular Docking and Biological Evaluation of Fused Thienopyrimidines and Quinazoline

Kaliraj, S., Jeyalakshmi, R., Kathiravan, M. K., Madhavan, T., & Devi, A. (2021) · Asian Journal of Chemistry · doi:10.14233/ajchem.2021.23062

Faculty Opinions recommendation of Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer.

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Metastasis Initiation

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Prediction of Drug-Target Binding Kinetics for Flexible Proteins by Comparative Binding Energy AnalysisPreprint

Nunes‐Alves, A., Ormersbach, F., & Wade, R. C. (2021) · ChemRxiv · doi:10.26434/chemrxiv.14208446

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Modulating pseudokinase conformation from the ATP-binding site

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BindingDB Entry 50012256: Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q23b63t8

BindingDB Entry 50011857: Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q24j0jrv

BindingDB Entry 50020002: Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy.

BindingDB (2024) · UC San Diego · doi:10.7270/q2kk9h7h

BindingDB Entry 50012115: Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q20005rj

BindingDB Entry 50040610: Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of

BindingDB (2013) · UC San Diego · doi:10.7270/q2z60q59

BindingDB Entry 50011751: Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.

BindingDB (2022) · UC San Diego · doi:10.7270/q2sj1q7g

BindingDB Entry 50018286: Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.

BindingDB (2024) · UC San Diego · doi:10.7270/q2tf02jj

BindingDB Entry 50043071: Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety.

BindingDB (2014) · UC San Diego · doi:10.7270/q27082sz

BindingDB Entry 50005908: KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.

BindingDB (2020) · UC San Diego · doi:10.7270/q2db84t7

BindingDB Entry 7843: Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.

BindingDB (2017) · UC San Diego · doi:10.7270/q23x85hp

BindingDB Entry 50013933: Discovery of a potent and selective Axl inhibitor in preclinical model.

BindingDB (2022) · UC San Diego · doi:10.7270/q2pv6q46

BindingDB Entry 50047219: Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.

BindingDB (2017) · UC San Diego · doi:10.7270/q2611258

BindingDB Entry 50047591: Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2.

BindingDB (2017) · UC San Diego · doi:10.7270/q28w3g6p

BindingDB Entry 50020773: Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.

BindingDB (2024) · UC San Diego · doi:10.7270/q2f47tmp

BindingDB Entry 50044636: Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer.

BindingDB (2016) · UC San Diego · doi:10.7270/q2jd4zcr

BindingDB Entry 50047059: Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.

BindingDB (2017) · UC San Diego · doi:10.7270/q2g73gmc

BindingDB Entry 7672: Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.

BindingDB (2017) · UC San Diego · doi:10.7270/q2td9w5m

BindingDB Entry 50010225: Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase.

BindingDB (2021) · UC San Diego · doi:10.7270/q2pn9949

BindingDB Entry 50001344: Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.

BindingDB (2020) · UC San Diego · doi:10.7270/q2mk6gdh

BindingDB Entry 50040754: Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.

BindingDB (2013) · UC San Diego · doi:10.7270/q2bp03xz

BindingDB Entry 50008257: Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.

BindingDB (2021) · UC San Diego · doi:10.7270/q27w6gkf

BindingDB Entry 50046221: Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2.

BindingDB (2016) · UC San Diego · doi:10.7270/q2sq9241

BindingDB Entry 50013982: Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.

BindingDB (2022) · UC San Diego · doi:10.7270/q2pr80sr

BindingDB Entry 50045394: Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold.

BindingDB (2016) · UC San Diego · doi:10.7270/q2vt1trt

BindingDB Entry 50042125: The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.

BindingDB (2013) · UC San Diego · doi:10.7270/q2xg9sd4

BindingDB Entry 50042523: Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.

BindingDB (2013) · UC San Diego · doi:10.7270/q21837vx

BindingDB Entry 50039744: Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

BindingDB (2013) · UC San Diego · doi:10.7270/q23b616c

BindingDB Entry 50002027: Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors.

BindingDB (2020) · UC San Diego · doi:10.7270/q2c53pf0

BindingDB Entry 50047507: AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.

BindingDB (2017) · UC San Diego · doi:10.7270/q24m96fs

BindingDB Entry 50043357: Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.

BindingDB (2014) · UC San Diego · doi:10.7270/q28g8n52

BindingDB Entry 50001529: Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors.

BindingDB (2020) · UC San Diego · doi:10.7270/q2v98bmq

BindingDB Entry 50044255: TBA

BindingDB (2015) · UC San Diego · doi:10.7270/q2hd7x6x

BindingDB Entry 50018884: Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer.

BindingDB (2024) · UC San Diego · doi:10.7270/q2d50s68

BindingDB Entry 50046292: Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.

BindingDB (2016) · UC San Diego · doi:10.7270/q28g8ng3

BindingDB Entry 50040382: Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

BindingDB (2013) · UC San Diego · doi:10.7270/q2df6s9n

BindingDB Entry 50000181: Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.

BindingDB (2019) · UC San Diego · doi:10.7270/q27p91jp

BindingDB Entry 50019130: Recent advances in the discovery of small molecule c-Met Kinase inhibitors.

BindingDB (2024) · UC San Diego · doi:10.7270/q2rf6097

BindingDB Entry 50019869: Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.

BindingDB (2024) · UC San Diego · doi:10.7270/q2vm4hp8

BindingDB Entry 50048116: Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.

BindingDB (2018) · UC San Diego · doi:10.7270/q2kk9dr0

BindingDB Entry 50046876: A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.

BindingDB (2017) · UC San Diego · doi:10.7270/q2vd719m

BindingDB Entry 50000692: Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.

BindingDB (2019) · UC San Diego · doi:10.7270/q22b91gs

BindingDB Entry 50047854: The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.

BindingDB (2018) · UC San Diego · doi:10.7270/q29g5pr8

BindingDB Entry 50034285: Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling.

BindingDB (2012) · UC San Diego · doi:10.7270/q2xk8fzt

BindingDB Entry 50006539: Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.

BindingDB (2020) · UC San Diego · doi:10.7270/q2qf8wvm

BindingDB Entry 50021678: Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy.

BindingDB (2025) · UC San Diego · doi:10.7270/q2tq6676

BindingDB Entry 7869: Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitors

BindingDB (2017) · UC San Diego · doi:10.7270/q2rj4h9q

BindingDB Entry 50043457: Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.

BindingDB (2014) · UC San Diego · doi:10.7270/q2br8tkw

BindingDB Entry 50043651: Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.

BindingDB (2014) · UC San Diego · doi:10.7270/q28w3frf

BindingDB Entry 50044858: Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.

BindingDB (2016) · UC San Diego · doi:10.7270/q2vm4dv8

Abstract 3613: Dual inhibitors against receptor tyrosine kinases c-Met and VEGFR-2 as efficacious antitumor agents in mouse xenograft tumor models

Wang, Q., Lu, W., Xing, X., Chen, M., Liu, Y., Zhao, L., Li, W., & Jiang, S. (2010) · Cancer Research · doi:10.1158/1538-7445.am10-3613

A Novel Inhibitor of c-Met and VEGF Receptor Tyrosine Kinases with a Broad Spectrum of In Vivo Antitumor Activities

Awazu, Y., Nakamura, K., Mizutani, A., Kakoi, Y., Iwata, H., Yamasaki, S., Miyamoto, N., Imamura, S., Miki, H., & Hori, A. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-1011 · Cited by 28

Inhibition of tumor cell growth, invasion, and metastasis by SIM-89, a novel inhibitor of HGF receptor tyrosine kinases.

Pei, J., Han, B., Shao, M., & Sha, H. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2012.30.15_suppl.e13528

Discovery and characterization of INCB028060, a novel, potent and selective Met RTK inhibitor for cancer treatment

Liu, X., Koblish, H. K., Wang, Q., Yang, G., Hall, L. M., Wen, X., Marando, C. A., Behshad, E., Wynn, R., Becker-Pasha, M., et al. (2008) · Cancer Research · Cited by 4

VEGF and c-Met Blockade Amplify Angiogenesis Inhibition in Pancreatic Islet Cancer

You, W., Sennino, B., Williamson, C. W., Falcón, B. L., Hashizume, H., Yao, L., Aftab, D. T., & McDonald, D. M. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-2527 · Cited by 262