Dasatinib is an orally-available, aminothiazole-based inhibitor of Abl and Src at IC50 values of 0.6 and 8 nm, respectively. [1] Dasatinib has been shown to be >300-fold more potent than imatinib in cells expressing wild-type Bcr-Abl and in a number of imatinib-resistant mutants at IC50s < 1.7 nM. [2] With the exception of T315I, Dasatinib inhibited cell proliferation of mutants in the range of 0.8 to 11 nM.

Dasatinib's activity against Lck allows for inhibition of T-cell receptor-mediated signal transduction, cellular proflieration, cytokine production, and in vivo T-cell responses. Combination of dasatinib with other immunomodulators such as cyclosporine A or rapamycin results in a synergistic inhibition of T-cell activation. [3]