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Table 1 List of HGF/c-MET inhibitors currently used in melanoma treatment with references to the in vitro, in vivo and clinical studies

From: Role of the HGF/c-MET tyrosine kinase inhibitors in metastasic melanoma

INHIBITOR Activity Use in melanoma treatment Refs
AMG-337 ATP-competitive, highly selective inhibitor of the c-Met receptor No [73]
AMG-458 Potent inhibitor of the c-Met, VEGFR-2, and IGF-I signaling pathways No [74]
Cabozantinib (XL184, BMS-907351) Inhibitor of tyrosine kinases including VEGF receptors, c-Met and AXL In vitro In vivo – clinical trial NCT00940225 NCT01835184 ([39, 87, 88], https://clinicaltrials.gov/ct2/show/NCT00940225, https://clinicaltrials.gov/ct2/show/record/NCT01835184)
Crizotinib (PF-02341066) Potent inhibitor of the c-Met and ALK In vitro In vivo – clinical trial NCT02223819 (uveal melanoma) (https://clinicaltrials.gov/ct2/show/NCT02223819, [89])
Foretinib (EXEL-2880) ATP-competitive inhibitor of the c-Met and VEGFR In vitro Animal study [78]
MK-2461 Multi-targeted inhibitor of the c-Met (WT/mutants), c-Met (Y1235D), c-Met (Y1230C), c-Met (N1100) No  
PF-04217903 Selective ATP-competitive c-Met inhibitor In vitro [90]
PHA-665752 Inhibitor of Y1234 and Y1235 in catalytic region of the c-Met In vitro [80, 81]
SU11274 Selective inhibitor of Y1234 and Y1235 in catalytic region of the c-Met In vitro Animal study [65, 66, 69]
Tivantinib (ARQ 197) Non-ATP-competitive c-Met inhibitor binding to the dephosphorylated c-Met kinase in vitro In vitro In vivo – clinical trial NCT00827177 ([66], https://clinicaltrials.gov/ct2/show/NCT00827177)