Fig 2. Series of EGFR-c-Src targeting type III molecules and their kinase inhibitory potency in vitro.

(A) EGFR-c-Src targeting type III molecules were designed and synthesized in our laboratory using quinazoline moieties (red) as the EGFR targeting head and dasatinib as the c-Src inhibitory arm (green), connected through different hydrolysable linkers. (B) In vitro kinase assay was used to determine the potency of each molecule in the series to competitively bind and inhibit the ATP binding pocket of the tyrosine kinase domains of EGFR and c-Src. Gefitinib and dasatinib were used as control drugs for comparison, and the IC₅₀ values of kinase inhibition were determined using the GraphPad Prism 6.0 software. Each value represents the average IC₅₀ from three independent experiments, carried out in duplicate.