Preferred Label : EGFR Mutant-specific Inhibitor CK-101;
NCIt related terms : OLAFERTINIB;
NCIt definition : An orally available third-generation and selective inhibitor of certain epidermal
growth factor receptor (EGFR) activating mutations, including the resistance mutation
T790M, and the L858R and del 19 mutations, with potential antineoplastic activity.
Upon administration, the EGFR mutant-specific inhibitor CK-101 specifically and covalently
binds to and inhibits selective EGFR mutations, with particularly high selectivity
against the T790M mutation, which prevents EGFR mutant-mediated signaling and leads
to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors,
CK-101 may have therapeutic benefits in tumors with T790M-mediated drug resistance.
This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause
dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors,
which also inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor
cell types, plays a key role in tumor cell proliferation and tumor vascularization.;
UNII : 708TLB8J3Y;
InChIKey : IDRGFNPZDVBSSE-UHFFFAOYSA-N;
CAS number : 1660963-42-7;
Molecule name : RX-518; CK 101; CK-101;
NCI Metathesaurus CUI : CL521020;
Origin ID : C132023;
UMLS CUI : C4329759;
Semantic type(s)
- concept_is_in_subset
- has_target
