Table 1.

In vitro kinase inhibition profile of cabozantinib

KinaseIC50 ± SD,a nmol/LEnzyme concentration, nmol/LATP concentration, μmol/LAssay
VEGFR20.035 ± 0.010.053A
MET1.3 ± 1.2101C
MET (Y1248H)3.8131C
MET (D1246N)11.8121C
MET (K1262R)14.6121C
RET5.2 ± 4.3152C
TIE214.3 ± 1.1155R
FLT311.3 ± 1.80.51C
KIT4.6 ± 0.513A
RON124 ± 1.2601C

Abbreviations: A, AlphaScreen; C, Coupled luciferase; R, radiometric; TBD, to be determined.

  • aMean ± SD of at least 3 independent determinations.