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. 2015 Aug 3;6(28):26090–26103. doi: 10.18632/oncotarget.4636

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: Inline graphic