Table 1.

Kinase inhibition profile of CH7057288

ClassEnzymeIC50 (nmol/L)
Tyrosine kinaseTRKA1.1 ± 0.12
TRKB7.8 ± 0.28
TRKC5.1 ± 1.1
INSR3,800 ± 670
ALK> 10,000
EGFR> 10,000
FGFR2> 10,000
FLT3> 10,000
HER2> 10,000
JAK2> 10,000
KDR> 10,000
MET> 10,000
ROS1> 10,000
SRC> 10,000
Serine/threonine kinaseAKT1> 10,000
CDK1> 10,000
CHK1> 10,000
CRAF> 10,000
ERK1> 10,000
PKA> 10,000
PKCα> 10,000
  • IC50 values of in vitro kinase assay were shown as mean ± standard deviation (n = 3).