Table 1.
Kinase selectivity profile of ZWM026
| Kinases | IC50 (mean ± SD)/nM |
|---|---|
| EGFR-T790M/L858R | 183.7±30.7 |
| EGFR-WT | 2429.0±396.1 |
| HER2 | 190.6±66.9 |
| HER3 | 160.3±32.2 |
| HER4 | 180.1±78.6 |
| RET | 279.6±58.6 |
| KDR | > 10000.0 |
| PDGFR-β | > 10000.0 |
| Flt-1 | > 10000.0 |
| ABL | > 10000.0 |
| EPH-A2 | > 10000.0 |
| RON | > 10000.0 |
| PDK1 | > 1000.0 |
| PDHK2 | > 1000.0 |
| PKBα | > 1000.0 |
| PI3K (p110α/p85α) | > 1000.0 |
| PKAcα | > 1000.0 |
| GSK3β | > 1000.0 |
| PKCα | > 1000.0 |
| PKCβI | > 1000.0 |
| PKCβII | > 1000.0 |
| PKCδ | > 1000.0 |
| PKCε | > 1000.0 |
| PKCη | > 1000.0 |
| PKCγ | > 1000.0 |
| PKCι | > 1000.0 |
| PKCμ | > 1000.0 |
| PKCν | > 1000.0 |
| PKCθ | > 1000.0 |
| PKCζ | > 1000.0 |
Note: shown are inhibitory activities of ZWM026 against a variety of kinases using an in vitro ELASA assay or provided by the Kinexus target profiling service. Some values are expressed as IC50 (mean ± SD) from three or more independent experiments.