Table 1.

Evaluation of TPX-0131 in biochemical assays of WT and mutant ALK variants.

KinaseIC50 (nmol/L)KinaseIC50 (nmol/L)KinaseIC50 (nmol/L)
WT1.4S1206R0.5T1151-L1152insT1.2
C1156Y0.2G1202R/L1198F0.6V1180L1.6
E1210K/S1206C0.2F1174L0.7G1269A1.6
L1198F/C1156Y0.2F1245C0.7F1174C1.8
L1196M/L1198F0.2R1275Q0.8I1171N2.3
E1210K0.3G1202R0.9L1152P2.9
L1196M0.3L1198F1.0D1203N4.4
T1151M0.4L1152R1.1D1203N/E1210K6.3
Deleted G12020.5F1174S1.2G1269S6.6
  • Note: The biochemical kinase assays were performed in the presence of 10 ╬╝mol/L ATP following previously described procedures (15).