Yao Cancer cell 2015
RAF inhibitors
WT RAF dimer 2
nd
site/V600E monomer
Vemurafenib
>135
Dabrafenib
83.4
Encorafenib
58.3
Concentration is needed to inhibit the second RAFwt dimer
In vitro
analysis of phospho-ERK inhibition in RAF dimers:
- The value reported in the table is
the fold change concentration needed to inhibit the second
dimer
in wild type healthy cells
RAF dimers inhibition