Table 4. Inhibitory activity of Raf inhibitors against Raf-1 (C-Raf) and A-Raf.
Assay Format | in vitro MAP2K1 phos. | KiNativ | |
---|---|---|---|
Enzyme Source | Recombinant | A375 | A375 |
Kinase | Raf-1 | Raf-1 | A-Raf |
sorafenib | 0.027 | >10 | >10 |
SB203580 | 1.8 | >10 | >10 |
GW5074 | 0.021 | >10 | >10 |
SB590885 | 0.025 | >10 | >10 |
PLX4720 | 0.012 | 0.35 | 0.022 |