Ability of NS-187 and imatinib to inhibit the phosphorylation of Bcr-Abl and other tyrosine kinases at the cellular level
. | . | IC50, nM . | . | |
|---|---|---|---|---|
| Tyrosine kinase . | Cell line . | NS-187 . | Imatinib . | |
| Bcr-Abl | ||||
| Wild type | 293T (transfected cells) | 22 | 1200 | |
| E255K | 293T (transfected cells) | 98 | > 10 000 | |
| T315I | 293T (transfected cells) | >10 000 | > 10 000 | |
| Bcr-Abl | ||||
| Wild type | BaF3 (transfected cells) | 63 | 491 | |
| E255K | BaF3 (transfected cells) | 340 | 6800 | |
| T315I | BaF3 (transfected cells) | > 10 000 | > 10 000 | |
| Bcr-Abl | K562 | 11 | 280 | |
| PDGFR | NHDF | 56 | 100 | |
| c-Kit | NCl-H526 | 840 | 210 | |
| EGFR | A431 | 3300 | > 10 000 | |
. | . | IC50, nM . | . | |
|---|---|---|---|---|
| Tyrosine kinase . | Cell line . | NS-187 . | Imatinib . | |
| Bcr-Abl | ||||
| Wild type | 293T (transfected cells) | 22 | 1200 | |
| E255K | 293T (transfected cells) | 98 | > 10 000 | |
| T315I | 293T (transfected cells) | >10 000 | > 10 000 | |
| Bcr-Abl | ||||
| Wild type | BaF3 (transfected cells) | 63 | 491 | |
| E255K | BaF3 (transfected cells) | 340 | 6800 | |
| T315I | BaF3 (transfected cells) | > 10 000 | > 10 000 | |
| Bcr-Abl | K562 | 11 | 280 | |
| PDGFR | NHDF | 56 | 100 | |
| c-Kit | NCl-H526 | 840 | 210 | |
| EGFR | A431 | 3300 | > 10 000 | |
K562 cells were examined for Bcr-Abl phosphorylation after treatment with NS-187 or imatinib by Western blot analysis with Bcr-Abl–specific antibodies, as were 293T or BaF3 cells transfected with wt or point mutants of Bcr-Abl. NHDF, NCl-H526, and A431 cells were examined for PDGFR, c-Kit, or EGFR phosphorylation, respectively, after treatment with first NS-187 or imatinib and then PDGF, SCF, or EGF, respectively, by Western blot analysis with the corresponding antibodies.