Description
As a potent and multi-targeted inhibitor, dasatinib (BMS-354825) can inhibit Abl, Src and c-Kit, with IC50 of <1 nM, 0.5 nM and 79 nM, respectively.
In vitro
As a potent and multi-targeted inhibitor, dasatinib (BMS-354825) can inhibit Abl, Src and c-Kit, with IC50 of (1) In HNSCC and NSCLC cells. In HNSCC and NSCLC cells, dasatinib induced cell cycle arrest by blocking the G1-S transition, and dasatinib can also result in apoptosis in some lines. By influencing Src and downstream mediators of adhesion, including focal adhesion kinase (FAK), p130, and paxillin, dasatinib showed effects on migration and invasion. By inducing p27 and the dephosphorylation of Rb, dasatinib showed effects on cell cycle and apoptosis. Dasatinib also induced morphologic changes that were consistent with an upstream role for Src in regulating focal adhesion complexes. (2) In human prostate cancer cells. Dasatinib blocks the kinase activities of the SFKs, Lyn, and Src, in human prostate cancer cells at low nanomolar concentrations. Focal adhesion kinase and Crk-associated substrate (p130(CAS)) signaling downstream of SFKs are also inhibited at similar concentrations of dasatinib. Dasatinib suppresses cell adhesion, migration, and invasion of prostate cancer cells at low nanomolar concentrations. (3) In imatinib-resistant cells. As a novel small molecule, Dasatinib showed potent inhibition to imatinib-resistant cell lines, malignant marrow cells isolated from patients with imatinib-resistant CML (chronic myeloid leukemia).
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