Table 5.

Alternate ABL kinase inhibitors with activity against KD mutants

IC50 cell proliferation, nM
CompoundClassWild-type BCR-ABLE255KM351TH396PT3151Reference no.
PD180970 Pyridopyrimidine 25 140 45 15 840 99
SKI DV-M016 Pyridopyrimidine ∼11 ∼30 NR ∼10 > 500 119
AP23848 Trisubstituted purine 14 94 24 8 9050 120
BMS-354825 2-amino-thiazole-5-carboxamide 0.087-1.000 Low nanomolar range Low nanomolar range Low nanomolar range > 1000 121,122
  • NR indicates not reported.