Table 1.

Comparison of the EC-70124 and midostaurin dissociation constants for selected kinases

Kd, nmol/L
KinaseEC-70124Midostaurin
FLT33.211
FLT3 (ITD)2.511
FLT3 (D835H)0.86.8
FLT3 (D835Y)1.115
FLT3 (D835V)0.82.2
FLT3 (N841I)1.46
FLT3 (K663Q)72
FLT3 (R834Q)1112
FLT3 (ITD, D835V)1.13.5
FLT3 (ITD, F691L)1.25
JAK19.4670
JAK22.594
JAK31.512
PDPK116190
PIM12.9560
PIM23.13,100
PIM30.4560
SYK888
KIT420220
PDGFRA140380
PDGFRB29110
  • NOTE: Assays run by Discoverex.