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Dissociation half-time of BRAF inhibitors
75
Compounds
Dissociation t
1/2
(hr)
Vemurafenib
0.5
Dabrafenib
2
Encorafenib
> 30
In vitro
analysis of BRAF kinase inhibition and half-time dissociation:
-
Dissociation half-time
is the time required to dissociate 50% of the drug from BRAF protein
in
vitro
à
reflects specificity of the drug
Koelblinger et al., Curr Opin Oncol. 2018