Table 1.
Differences in the IC50 of TKIs tried or approved to treat STS (μmol/L).
| Tyrosine Kinase | Pazopanib [33] | Sorafenib [55,56] | Sunitinib [56,57] | Cediranib [56] | Regorafenib [56,57,58,59] |
|---|---|---|---|---|---|
| VEGFR-1 | 0.01 | - | 0.002 | 0.005 | 0.013 |
| VEGFR-2 | 0.03 | 0.09 | 0.009 | <0.001 | 0.0042 |
| VEGFR-3 | 0.047 | 0.02 | 0.017 | <0.003 | 0.046 |
| PDGFR-α | 0.071 | - | 0.069 | - | 0.136 |
| PDGFR-β | 0.084 | 0.057 | 0.002 | 0.005 | 0.022 |
| c-Kit | 0.074 | 0.068 | 0.022 | 0.002 | 0.007 |
| FGFR-1 | 0.14 | 0.58 | 0.88 | - | 0.202 |
| FGFR-3 | 0.13 | - | - | - | - |
| FGFR-4 | 0.8 | - | - | - | - |
| c-fms | 0.146 | - | - | - | - |
| LCK | 0.411 | - | - | - | - |
| ITK | 0.43 | - | - | - | - |
| FAK | 0.8 | - | - | - | - |
| p38α | 1.056 | - | - | - | - |
| Abl1 | 2 | - | - | - | - |
| JNK1 | 2.466 | - | - | - | - |
| Ret | 2.8 | - | - | - | 0.0015 |
| Src | 3.09 | - | - | - | - |
| GSK3 | 3.46 | - | - | - | - |
| JNK3 | 4.065 | - | - | - | - |
| ALK6 | 4.266 | - | - | - | - |
| Tie-2 | 4.52 | - | - | - | - |
| Met | 6 | - | - | - | - |
| IGF-1R | 8 | - | - | - | - |
| CSF-1R | - | - | 0.05–0.10 | - | - |
| JNK2 | 10.233 | - | - | - | - |
| Flt-3 | >20 | 0.058 | 0.25 | >1 | - |
| Raf | - | 0.006 | - | - | - |