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. Author manuscript; available in PMC: 2012 Jun 26.
Published in final edited form as: Chem Biol. 2011 Jun 24;18(6):699–710. doi: 10.1016/j.chembiol.2011.04.011

Table 4. Inhibitory activity of Raf inhibitors against Raf-1 (C-Raf) and A-Raf.

Several Raf inhibitors were evaluated against Raf-1 and A-Raf endogenously expressed in A375 cells and against recombinant Raf-1 in an in vitro phosphorylation assay. See also Supplemental Figure S5 and Supplemental Tables S5 and S6.

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