Preferred Label : FAK/ALK/ROS1 Inhibitor APG-2449;
NCIt related terms : APG-2449;
NCIt definition : An orally available kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma
kinase (ALK), focal adhesion kinase (FAK) and the receptor tyrosine kinase C-ros oncogene
1 (ROS1), with potential antineoplastic activity. Upon administration, ALK/FAK/ROS1
inhibitor APG-2449 selectively binds to and inhibits ALK, FAK and ROS1 kinases. The
inhibition leads to disruption of ALK-, FAK- and ROS1-mediated signal transduction
pathways and eventually inhibits tumor cell growth in ALK-, FAK- and ROS1-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. ROS1, overexpressed in certain cancer cells, plays a key role in cell
growth and survival of cancer cells.;
UNII : 8L976E3N4N;
Molecule name : APG-2449; APG 2449;
NCI Metathesaurus CUI : CL1406284;
Origin ID : C172193;
UMLS CUI : C5417900;
Semantic type(s)
- concept_is_in_subset
