CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src ( IC 50 s of 5-20 and 40 nM, respectively),and also inhibits Src , EGFR , KDR , v-Abl, and Lck with IC 50 s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.