Preferred Label : EGFR/VEGFR/RET Inhibitor HA121-28;
NCIt definition : An orally available inhibitor of the epidermal growth factor receptor (EGFR), the
proto-oncogene receptor tyrosine kinase rearranged during transfection (RET) and vascular
endothelial growth factor receptor (VEGFR), with potential anti-angiogenic and antineoplastic
activities. Upon oral administration of HA121-28, this agent targets, binds to and
inhibits the activity of EGFR, RET and VEGFR. This prevents EGFR-, RET- and VEGFR-mediated
signaling, and may lead to the induction of apoptosis and inhibition of tumor growth
in EGFR-, RET- and VEGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated
in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
Dysregulation of RET activity plays a key role in the development and progression
of a variety of cancers. Expression of VEGFR is upregulated in a variety of tumor
cell types; it plays a key role in the migration, proliferation and survival of endothelial
cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor
cell death.;
Molecule name : HA 121-28; HA121-28; HA-121 28;
NCI Metathesaurus CUI : CL1407411;
Origin ID : C173436;
UMLS CUI : C5417983;
Semantic type(s)
concept_is_in_subset