NCIt definition : An orally bioavailable focal adhesion kinase (FAK) inhibitor with potential antineoplastic
activity. Upon administration, VS-4718 inhibits FAK, blocks fibronectin-stimulated
FAK autophosphorylation of Tyr397, and may prevent the integrin-mediated activation
of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt.
This results in the reduction of the number of cancer stem cells (CSCs) and inhibits
tumor cell migration, proliferation and survival. The cytoplasmic tyrosine kinase
FAK is a signal transducer for integrins and is constitutively activated in various
tumor cell types; it is involved in tumor cell invasion, migration and proliferation
and plays a key role in the development, function and survival of CSCs.;
See also inter- (CISMeF)