Table 1.

WT and mutant KIT: kinase activity of activated proteins and affinity of sunitinib for unactivated proteins

ProteinKinase activity of activated proteins
Unactivated proteins
ATP Km, μMkcat, s−1kcat/Km, s−1M−1SU IC50, μMSU Kd*, nM
WT42.51.6739,2942120 ± 13
D816H22.01.2958,636>3022 ± 15
D816V17.00.5532,559>3013 ± 6
V560D35.01.4741,857254.4 ± 0.6
V654A13.51.2693,3338.6ND
V560D + T670I12.80.9675,156>3014 ± 9
  • cat, catalytic; SU, sunitinib; ND, not determined.

  • *Determined by using the Trp fluorescence quench assay.