Alternate ABL kinase inhibitors with activity against KD mutants
. | . | IC50 cell proliferation, nM . | . | . | . | . | . | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Compound . | Class . | Wild-type BCR-ABL . | E255K . | M351T . | H396P . | T3151 . | Reference 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 | ||||
. | . | IC50 cell proliferation, nM . | . | . | . | . | . | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Compound . | Class . | Wild-type BCR-ABL . | E255K . | M351T . | H396P . | T3151 . | Reference 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.