Dasatinib

Dasatinib is a potent multi-kinase inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family. Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (Ki values are 16 and 30 pM, respectively). It is also effective at sub-nanomolar concentrations, inhibiting Lyn, Fyn, EPHA2, PDGFR, c-Kit, Lck and Yes. At nanomolar concentrations, Dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants. Dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease. It suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carcinoma and non-small cell lung cancer cells. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model. Dasatinib shows immunosuppressive, senolytic and antiviral properties. Dasatinib inhibits replication of SARS-CoV and MERS-CoV in vitro (EC50 = 2.1 and 5.5 µM, respectively) and shows also activity against Denuge virus and SARS-CoV-2.