Table 1.

Kinase selectivity profile of CHIR-124

KinaseIC50 (μmol/L)
Cell cycle kinases
    CHK1 KD0.0003
    CHK20.6974
    Cdk4/cyclin D2.05
    CDC2/cyclin B0.5057
    Cdk2/cyclin A0.1911
Receptor tyrosine kinases
    cMET>3
    bFGFR2.01
    FGFR31.29
    VEGFR2 FLK10.5779
    VEGFR1 FLT10.4636
    PDGFR0.0066
    FLT30.0058
Serine/threonine kinases
    PKCα0.58
    PKAβ I2.25
    PKCβ II0.58
    PKCγ0.11
    ERK24.31
    PKA0.1031
    GSK30.0233
Non–receptor tyrosine kinases
    CABL14.88
    LCK0.1583
    FYN0.0988
  • Abbreviations: KD, kinase domain; Cdk2, cyclin-dependent kinase 2; bFGFR, basic fibroblast growth factor receptor; PKC, protein kinase C; VEGFR, vascular endothelial growth factor receptor; ERK, extracellular signal-regulated kinase.