Table 1.

The IC50 of pazopanib against the indicated enzyme in a cell-free assay system

EnzymeKinase IC50 (μmol/L)
VEGFR10.010
VEGFR20.030
VEGFR30.047
PDGFRα0.071
PDGFRβ0.084
c-Kit0.074
FGFR10.14
FGFR30.13
FGFR40.8
c-fms0.146
LCK0.411
ITK0.430
FAK0.8
p38α1.056
Abl12
JNK12.466
Ret2.8
Src3.090
GSK33.460
JNK34.065
ALK64.266
Tie-24.520
Met6
IGF-IR8
JNK210.233
Akt3; CDK1 and CDK2; EphB4; ErbB1, ErbB2, and ErbB4; Flt-3; INS-R; PLK1 and PLK3; PKC-β1 and PKC-β2; Syk; Wee1>20
  • Abbreviations: LCK, lymphocyte-specific protein tyrosine kinase; ITK, interleukin-2–inducible T-cell kinase; FAK, focal adhesion kinase; JNK1, JNK2, and JNK3, c-jun NH2-terminal kinases 1, 2, and 3; GSK3, glycogen synthase kinase 3; ALK6, activin-like kinase 6; IGF-IR, insulin-like growth factor type I receptor; CDK1 and CKD2, cyclin-dependent kinases 1 and 2; INS-R, insulin receptor; PLK1 and PLK3, polo-like kinases 1 and 3; PKC-β1 and PKC-β2, protein kinase C-β1 and -β2.