Src kinase inhibitor I

Src kinase inhibitor I is a 4-anilinoquinazole competitive inhibitor of Src family tryosine kinases. Src kinase inhibitor I is a dual site inhibitor, described to compete at both the ATP and peptide binding sites of the kinase. A particularly potent inhibitor of the Src kinases, Src Kinase inhibitor I demonstrates nanomolar inhibition of c-Src (IC₅₀ = 44 nM) and Lck (IC₅₀ = 88 nM). Low micromolar inhibition of Flk-1 (VEGFR2, IC₅₀ = 0.32 μM) and C-fms (IC₅₀ = 30 μM) are also reported. Src Kinase inhibitor I demonstrates a strong selectivity for Src over the other kinases, a property attributed to the dual site inhibition action of this compound. Use of Src Kinase inhibitor I in parallel with PP 1 and PP 2 for Src family kinase inhibition has also been described.