Preferred Label : Pan-variant KIT Inhibitor THE-630;
NCIt synonyms : KIT-mutant Inhibitor THE-630; Pan-KIT-mutant Inhibitor THE-630; Pan-KIT Inhibitor THE-630;
NCIt definition : An orally bioavailable pan-inhibitor of the mutated forms of the tumor-associated
antigen (TAA) receptor tyrosine kinase mast/stem cell factor receptor c-Kit (SCFR),
with potential antineoplastic activity. Upon oral administration, pan-variant KIT
inhibitor THE-630 targets, binds to and inhibits the activity of all known, clinically
relevant KIT activating and resistance mutations in gastrointestinal stromal tumors
(GIST). More specifically, THE-630 inhibits the primary activating mutations deletion
in Ex11 (Ex11Del) and insertion in Ex9 (Ex9Ins); the secondary resistance mutations,
including the ATP binding pocket mutants V654A and T670I and the activation loop mutants
D816G/H, D820A/G, N822K, Y823D, and A829P. This inhibits KIT-mediated signaling and
the proliferation of tumor cells that overexpress c-Kit mutations. c-Kit is mutated
in various tumor cell types and plays a key role in the regulation of cellular proliferation
and resistance to chemotherapy.;
Molecule name : THE 630; THE-630;
NCI Metathesaurus CUI : CL1773952;
Origin ID : C185596;
UMLS CUI : C5576915;
Semantic type(s)
- concept_is_in_subset
- has_target
