Preferred Label : c-Met Inhibitor ANS014004;
NCIt definition : An orally bioavailable, next-generation, type II inhibitor of the oncoprotein c-Met
(hepatocyte growth factor receptor; HGFR), with potential antineoplastic activity.
Upon oral administration, c-Met inhibitor ANS014004 selectively targets and specifically
binds to the inactive state of c-Met (DFG-out) in the ATP pocket and inhibits the
activity of the c-Met protein, including various c-Met oncogenic alterations such
as MET exon 14 skipping mutation (METdeltaex14) and acquired mutations in codons D1228
and Y1230. This prevents c-Met phosphorylation and disrupts c-Met-dependent signal
transduction pathways. This may induce cell death in and inhibit proliferation of
tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met
protein. c-Met protein is overexpressed or mutated in many tumor cell types and plays
key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.
Type II c-Met inhibitors may overcome resistance to type I c-Met inhibitors. Post-treatment
resistance to type I c-Met inhibitors often occurs through acquired mutations in codons
D1228 and Y1230.;
Molecule name : ANS-014004; ANS 014004; ANS 01; ANS-01;
NCI Metathesaurus CUI : CL1928790;
Origin ID : C206697;
concept_is_in_subset
- has_target
