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) | |
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 | Â |
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 | |
SU11274 | Selective inhibitor of Y1234 and Y1235 in catalytic region of the c-Met | In vitro Animal study | |
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 |