Table 2.
In vitro protein kinase inhibition of compounds 6c and 6h-j against EGFR, Her2, VEGFR2, CDK2, AURKC, HDAC1, and mTOR.
| Compound | In Vitro Protein Kinase Inhibition IC50 (nM) | ||||||
|---|---|---|---|---|---|---|---|
| EGFR | Her2 | VEGFR2 | CDK2 | AURKC | HDAC1 | mTOR | |
| 6c | 125.2 ± 0.041 | 55.6 ± 0.023 | 604.5 ± 0.022 | 938 ± 0.039 | 94.4 ± 0.036 | 2263 ± 0.077 | 1461 ± 0.05 |
| 6h | 73.2 ± 0.004 | 23.2 ± 0.001 | 194.5 ± 0.007 | 284 ± 0.012 | 11 ± 0.004 | 151.1 ± 0.005 | 413 ± 0.014 |
| 6i | 30.1 ± 0.03 | 28.3 ± 0.001 | 172.2 ± 0.006 | 364 ± 0.011 | 74.5 ± 0.003 | 96.6 ± 0.003 | 152 ± 0.005 |
| 6j | 166.4 ± 0.008 | 204.7 ± 0.009 | 307.2 ± 0.011 | 1448 ± 0.062 | 589.4 ± 0.022 | 473.3 ± 0.016 | 1305 ± 0.044 |
| Erlotinib | 61.1 ± 0.002 | - | - | - | - | - | - |
| Lapatenib | - | 17.4 ± 0.001 | - | - | - | - | - |
| Sorafenib | - | - | 45.4 ± 0.002 | - | - | - | - |
| Roscovetine | - | - | - | 756 ± 0.032 | - | - | - |
| TSA | - | - | - | - | 30.4 ± 0.001 | 37.4 ± 0.001 | - |
| Rapamycin | - | - | - | - | - | - | 208 ± 0.007 |
IC50 values are the mean ± SD of triplicate measurements.