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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