Table 1. Effect of Src inhibitors on EGFR TK catalytic activity.
EGFR d746-750 | EGFR d747-749 A750P | EGFR d747-752 P753S | EGFR d752-759 | EGFR G719C | EGFR G719S | EGFR L858R | EGFR L861Q | EGFR T790M | EGFR T790M/L858R | EGFR wt | |
---|---|---|---|---|---|---|---|---|---|---|---|
Compound | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) | IC50 (nM) |
Saracatinib | 13.1 | 13.3 | 10.0 | 36.2 | 9.77 | 13.5 | 9.40 | 12.3 | 769 | 802 | 11.0 |
Dasatinib | 54.7 | 64.0 | 61.2 | 138 | 24.8 | 21.7 | 28.1 | 25.5 | 3100 | 2790 | 25.4 |
Bosutinib | 2.53 | 5.80 | 3.47 | 23.7 | 2.59 | 2.25 | 2.29 | 3.95 | 145 | 214 | 3.17 |
Erlotinib | 1.56 | 2.40 | 1.57 | 2.33 | 2.30 | 2.22 | 1.62 | 1.24 | 200 | 999 | 1.01 |
Compound concentrations in the assay from 0.3 nM to 10 μM, semi-log steps; singlicate measurement Ranking of IC50 values: