AP23464 IC50 (nM) values for cellular proliferation, cellular Bcr-Abl tyrosine phosphorylation, GST-Abl kinase autophosphorylation, and GST-Abl kinase peptide substrate phosphorylation
. | AP23464 IC50, nM . | . | . | . | |||
|---|---|---|---|---|---|---|---|
| . | Ba/F3 cellular assays . | . | Purified GST-Abl kinase assays . | . | |||
. | Cellular proliferation . | Bcr-Abl tyrosine phosphorylation . | Autophosphorylation . | Peptide substrate . | |||
| Vector only | 8275 | — | — | — | |||
| Wild type | 14 | 13 | 61 | 6 | |||
| Q252H | 18 | 12 | ND | ND | |||
| Y253F | 26 | 28 | 54 | 13 | |||
| E255K | 94 | 57 | 110 | 14 | |||
| T3151 | 9050 | > 5000 | > 5000 | > 5000 | |||
| M351T | 24 | 30 | 31 | 8 | |||
| H396P | 8 | 9 | 54 | 11 | |||
. | AP23464 IC50, nM . | . | . | . | |||
|---|---|---|---|---|---|---|---|
| . | Ba/F3 cellular assays . | . | Purified GST-Abl kinase assays . | . | |||
. | Cellular proliferation . | Bcr-Abl tyrosine phosphorylation . | Autophosphorylation . | Peptide substrate . | |||
| Vector only | 8275 | — | — | — | |||
| Wild type | 14 | 13 | 61 | 6 | |||
| Q252H | 18 | 12 | ND | ND | |||
| Y253F | 26 | 28 | 54 | 13 | |||
| E255K | 94 | 57 | 110 | 14 | |||
| T3151 | 9050 | > 5000 | > 5000 | > 5000 | |||
| M351T | 24 | 30 | 31 | 8 | |||
| H396P | 8 | 9 | 54 | 11 | |||
ND indicates not done; —, not applicable.