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BRAF inhibitors have different kinase inhibition activity
Encorafenib inhibits BRAFwt, BRAFv600E and CRAF in the same way and with a lower
IC50 than other BRAF inhibitors
Inhibitor
Biochemical
BRAF
IC
50
(
µ
M)
BRAFV600E
IC
50
(
µ
M)
CRAF
IC
50
(
µ
M)
Encorafenib
1
0.0005
0.0004
0.0003
Dabrafenib
2
0.0032
0.0006
0.005
Vemurafenib
3
0,11
0.035
0,048
1.
Stuart DD, et al. AACR. 2012: abstract 3790
2.
King AJ, et al. PLoS ONE 8:e67583
3.
Poulikakos et al. Nature, 2010
Inhibition of RAF kinase
in vitro
:
IC50:
Concentration which inhibits 50% of kinase activity
in vitro
RAS
Healthy cells
BRAF
wt
CRAF
or
BRAF
BRAF
Dimerization
CRAF or
BRAF
BRAF
P
P
P
PP
P
P
P
RTK
Encorafenib
Encorafenib