Table 1.
Kinase activity and selectivity of BI 853520
| BI 853520 | PF-562,271 | |
|---|---|---|
| Kinase IC50 [nM] | ||
| PTK2/FAK (DELFIA®) | 1 | 2 |
| PTK2/FAK (Z-'LYTE®) | 38.1 | 29.7 |
| Selectivity (number of kinases hit ≤50% control at 1000 nM/total kinases) | ||
| 4/262 | 15/37 | |
| Kinase IC50 [nM] | ||
| PTK2B/PYK2 (DELFIA®) | >50,000 | 22 |
| PTK2B/PYK2 (Z’-LYTE®) | 2000 | 48 |
| FER (Z'-LYTE®) | 903 | n.d. |
| FES (Z'-LYTE®) | 1040 | n.d. |
| PAK7 (Z'-LYTE®) | >10 000 | n.d. |
Overview of in vitro kinase activity and selectivity of BI 853520 and PF-562,271. Two different assay formats were used to determine IC50 values for inhibition of FAK and PYK2. Selectivity was determined on a larger kinase panel at a concentrations of 1000 nmol/L, for kinase hits from this screen IC50 values were measured for BI 853520
n.d. not determined