Table 3. Cell growth inhibition by PTK6 inhibitors in PTK6-positive tumor cells and PTK6-negative HEK293T cells.
| Cell line | PTK6/p-PTK6 expression | 21a, IC50 (uM) | PF-6698840, IC50 (uM) | ||
|---|---|---|---|---|---|
| 3D culture | 2D culture | 3D culture | 2D culture | ||
| HEK293T | -/- | 6.1 ± 3.1 | 7.3 ± 3.2 | 17 ± 10 | 17 ± 10 |
| MDA-MB-231 | +/++ | 15 ± 9 | 18 ± 9 | >10 | >10 |
| MDA-MB-453 | +/+ | 6.4 ± 2.4 | 6.6 ± 3.4 | >20 | >20 |
| T47D | ++/+ | >10 | >10 | 9 ± 3 | 7 |
The compound potency IC50 was determined by non-linear regression curve fitting to a dose-response equation in Graphpad Prism. The IC50 values were similar in 2D and 3D cultures and described as the average ± standard deviation.
The relative expression levels of PTK6 and p-PTK6 in cells are indicated with ++ as highest level, and–as undetectable level.