Table 1. Cellular mechanistic IC50 values for OXA-11 inhibition of FAK and other kinases in cell lysates.
| Kinase | OXA-11 IC50 (nM) | Fold selectivity for FAK |
|---|---|---|
| FAK | 10 | 1× |
| PYK2 | 80 | 8× |
| RSK1/2 | 260 | 26× |
| Aurora kinase A | >10,000 | >1000× |
| Aurora kinase B | >10,000 | >1000× |
| Insulin receptor | >10,000 | >1000× |
| SRC | >10,000 | >1000× |
| KDR | >10,000 | >1000× |
Cell-based kinase assays were done to determine the IC50 values (nM) for OXA-11 inhibition of these kinases in cell lysates using Omnia Kinase Assays (Invitrogen)