Background:

Dasatinib is a small-molecule inhibitor of both the Src and Bcr-Abl tyrosine kinases with IC₅₀?values of 0.5 nM and 1 nM. ?The oncogenic tyrosine kinase Bcr-Abl, plays a critical role in the pathogenesis of CML?(chronic myelogenous leukemia). In most CML patients, the kinase domain of Bcr-Abl have mutations that interfere with binding to the first Abl kinase inhibitor, but Dasatinib bind more efficiently to these Abl kinase mutations and thus more effective than imatinib in inhibiting the proliferation cells with wild-type Bcr-Abl or Bcr-Abl mutants.

参考文献
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