Table 1.
Comparison of in vitro biochemical kinase inhibition by regorafenib and sorafenib
| Kinase target | Regorafenib8 (IC50 [nM/L]) |
Sorafenib9 (IC50 [nM/L]) |
|---|---|---|
| VEGFR-1 | 13 | N/A |
| VEGFR-2 | 4.2 | 15 |
| VEGFR-3 | 46 | 20 |
| TIE-2 | 311 | N/A |
| PDGFR-β | 22 | 57 |
| FGFR1 | 202 | 580 |
| BRAF | 28 | 22 |
| BRAFV600E | 19 | 38 (V599E) |
Note: VEGFR-2/3 are murine VEGFRs.
Abbreviations: FGFR, fibroblast growth factor receptor; IC50, 50% inhibitory concentration; N/A, not available; PDGFR, platelet-derived growth factor receptor; TIE-2, tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2; VEGFR, vascular endothelial growth factor receptors.