Effect of NS-187 and imatinib on the in vitro phosphorylation of purified wt and point mutated Abl kinase domains
. | IC50, nM . | . | |
|---|---|---|---|
| Abl kinase . | NS-187 . | Imatinib . | |
| Wild type | 72 | 1 100 | |
| M244V | 240 | 3 500 | |
| G250E | 160 | 2 000 | |
| Q252H | 410 | 2 100 | |
| Y253F | 81 | 1 500 | |
| E255K | 540 | 5 800 | |
| E255V | 1 400 | > 10 000 | |
| T315I | > 10 000 | > 10 000 | |
| F317L | 760 | 1 900 | |
| M351T | 150 | 3 900 | |
| E355G | 580 | 7 100 | |
| E359V | 1 300 | > 10 000 | |
| H396P | 95 | 1 400 | |
| F486S | 470 | 9 500 | |
. | IC50, nM . | . | |
|---|---|---|---|
| Abl kinase . | NS-187 . | Imatinib . | |
| Wild type | 72 | 1 100 | |
| M244V | 240 | 3 500 | |
| G250E | 160 | 2 000 | |
| Q252H | 410 | 2 100 | |
| Y253F | 81 | 1 500 | |
| E255K | 540 | 5 800 | |
| E255V | 1 400 | > 10 000 | |
| T315I | > 10 000 | > 10 000 | |
| F317L | 760 | 1 900 | |
| M351T | 150 | 3 900 | |
| E355G | 580 | 7 100 | |
| E359V | 1 300 | > 10 000 | |
| H396P | 95 | 1 400 | |
| F486S | 470 | 9 500 | |
The purified Abl kinase domains were subjected to in vitro kinase assays as described in “Materials and methods.” The enzyme concentration was 10 nM.