Table 3.
In Vitro Enzymatic Activity of 3b Against Various Receptor Tyrosine Kinases (IC50 in μM).a
| Compound | EGFR | VEGFR2 | c-Met | IGF1R | c-Src | JAK2 |
|---|---|---|---|---|---|---|
| 1 | – | – | – | 0.10b | 0.42b | 1.07b |
| 3b | >10 | >10 | >10 | 4.84 | 3.38 | >10 |
| Staurosporine | 0.16 | 0.021 | 0.18 | 0.041 | 0.0025 | 0.0004 |
a
Data from Reaction Biology Corporation. Compounds were tested in duplicate in ten-dose IC50 mode with three-fold serial dilutions starting at 10 μM. Control compound (staurosporine) was tested in ten-dose IC50 mode with three-fold serial dilutions starting at 20 μM. Reactions were carried out at 20 μM ATP. Average values are shown.
b
Data from reference.35