Table 2.

WT and mutant KIT: inhibition by sunitinib and rates of auto-activation

ProteinSunitinib IC50 (μM)
Activation rate
Unactivated KIT
Activated KIT
1 h4 h16 h1 hmM−1s−1× WT
WTLow signal0.040.0421.000.251
D816H0.213.20>10.00>30.0046184
D816V7.10>10.00>10.00>30.00134536
V560D0.020.170.2425.00>150>600
V654A0.010.080.158.604.819
V560D + T670I0.040.280.36>30.00>150>600
ΔJM0.030.160.53>30.00NDND