Table 1. Inhibition of CDK2, PI3K and mTOR kinases by 6-aminopyrimidines.
| Compound | CDK2 | PI3Kα | PI3kβ | PI3Kδ | PI3Kγ | mTOR |
|---|---|---|---|---|---|---|
| 1 | 0.0001±0.00003 | 3.6, 6.2 | >20 | 3.2, 7.5 | 3.7, 6.8 | >20 |
| 2 | 2.2±0.5 | 1.3, 2.7 | 5.7, 11 | 0.7, 1.8 | 1.5, 2.1 | 19 |
| 7 | 9.6, 13 | 9.9, 12 | >20 | 12, 14 | 18, 20 | >20 |
| 6 | 7.5, 22 | 2.9, 4.4 | >20 | 5.0, 6.5 | 2.9, 7.1 | >20 |
| 4 | 22, 24 | 5.4, 11 | >20 | 2.9, 5.6 | 1.7, 5.3 | 15 |
| 5 | 60±10 | 4.5, 7.7 | 18, 23 | 6.9, 5.9 | 7.5, 12 | >20 |
| 8 | >>10 | 2.5, 6.2 | 4.3, 13 | 0.5, 1.1 | 1.5, 2.0 | 4.9 |
| 3 | >>10 | >20 | >20 | >20 | >20 | 13 |
Abbreviations: mTOR=mammalian target of rapamycin; PI3K=phosphatidylinositol-3-kinase. Values are the IC50 (μM) or the highest concentration tested (μM), and are the mean±s.d. or individual determinations. For chemical structures see Supplementary Figure 1.