NCIt definition : An orally available dual kinase inhibitor of the receptor tyrosine kinase anaplastic
lymphoma kinase (ALK) and focal adhesion kinase (FAK), with potential antineoplastic
activity. Upon administration, ALK-FAK inhibitor CEP-37440 selectively binds to and
inhibits ALK kinase and FAK kinase. The inhibition leads to disruption of ALK- and
FAK-mediated signal transduction pathways and eventually inhibits tumor cell growth
in ALK- and FAK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily
and plays an important role in nervous system development; its dysregulation and gene
rearrangements are associated with a variety of tumors. The cytoplasmic tyrosine kinase
FAK, a signal transducer for integrins, is upregulated and constitutively activated
in various tumor types; it plays a key role in tumor cell migration, proliferation,
survival, and tumor angiogenesis.;