Table 1. Effect of everolimus on Met TK catalytic activity.
| D1228H | D1228N | F1200I | M1250T | Wild-type | Y1230A | Y1230C | Y1230D | Y1230H | |
|---|---|---|---|---|---|---|---|---|---|
| Compound | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) | IC50 (μM) |
| everolimus | >10 | >10 | >10 | >10 | >10 | >10 | >10 | >10 | >10 |
| PHA665752 | 4.37 | 6.35 | 0.734 | 0.108 | 0.0185 | 4.22 | 3.57 | 7.92 | 1.88 |
Compound concentrations in the assay from 0.3 nM to 10 μM, semi-long step, singlicate measurement.
Ranking of IC50 values:
| IC50 (μM) above 10 | |
| IC50 (μM) between 10 and 1 | |
| IC50 (μM) between 1 and 0.1 | |
| IC50 (μM) below 0.1 |