Table 1.
Inhibitors of HGF/c-MET signaling investigated in melanoma cells, in preclinical and clinical studies.
| Name of Inhibitor | Designed/Assessed Activity | Type of Experiments | References |
|---|---|---|---|
| CabozantinibXL184 BMS-907351 |
Inhibitor of c-MET | Clinical trial |
NCT00940225 [123,138,139] |
| Crizotinib PF-02341066 |
Adenosine triphosphate (ATP)-competitive inhibitor of catalytic activity of c-MET | Preclinical in vivo clinical trial (uveal melanoma) |
[103,124] NCT02223819 (ongoing) |
| Foretinib EXEL-2880 |
ATP-competitive inhibitor of c-MET | Preclinical in vitro Preclinical in vivo |
[128] |
| PHA-665752 | Inhibitor of Y1234 and Y1235 in catalytic region of c-MET | Preclinical in vitro | [129,130] |
| SU11274 | Selective inhibitor of Y1234 and Y1235 in catalytic region of c-MET | Preclinical in vitro Preclinical in vivo |
[86,115,125,126,127] |
| Tivantinib ARQ 197 |
Non-ATP-competitive inhibitor of c-MET; binding to dephosphorylated c-MET | Preclinical in vitro Preclinical in vivo Clinical trial |
[126,131,132,133] NCT00827177 |
| E7050 | ATP-competitive inhibitor of c-MET | Clinical trial | NCT01433991 |
| Quercetin | Inhibitor of c-MET phosphorylation and dimerization | Preclinical in vitro Preclinical in vivo |
[36,135] |