zinc 1488120

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.

CGP77675 hydrate is an orally active, potent inhibitor of Src family kinases. It inhibits the phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively), as well as Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate may be useful for treating diseases associated with elevated bone loss and has anticancer activity [1].