NCIt definition : An orally bioavailable inhibitor of checkpoint kinase 2 (chk2), with potential antineoplastic
and chemopotentiating activities. Upon oral administration, lasmotinib binds to and
inhibits the activity of chk2, which may prevent the repair of DNA damage caused by
DNA-damaging agents. This may result in tumor cell apoptosis and potentiate the antitumor
efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine
kinase, is a key component in the DNA replication-monitoring checkpoint system and
is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by
a variety of cancer cell types.;
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