Dasatinib

Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.{24166,24167} It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.{24166,24156,24168} At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.{24156,24168} Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.{24166,24164,17350,17482}