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- NCIT_C187042 IAO_0000115 "An orally bioavailable, central nervous system (CNS) penetrating, mutant-selective covalent inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion (Ex20ins) activating mutations, with potential antineoplastic activity. Upon oral administration, EGFR Ex20ins inhibitor BLU-451 selectively targets, irreversibly binds to and inhibits the activity of EGFR Ex20ins and some other oncogenic point mutations. This prevents EGFR Ex20ins-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR Ex20ins-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumors, plays a key role in tumor cell proliferation and tumor vascularization. BLU-451 is able to penetrate the blood-brain-barrier (BBB) and may therefore exert its activity against EGFR Ex20ins-driven CNS primary tumors and CNS metastases. BLU-451 does not inhibit the activity of wild-type (WT) EGFR. EGFR Ex20ins are oncogenic driver mutations that constitutively upregulate kinase activity." @default.
- NCIT_C187042 NCIT_A7 NCIT_C125605 @default.
- NCIT_C187042 NCIT_A7 NCIT_C17068 @default.
- NCIT_C187042 NCIT_NHC0 "C187042" @default.
- NCIT_C187042 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C187042 NCIT_P108 "EGFR Exon 20 Insertion Inhibitor BLU-451" @default.
- NCIT_C187042 NCIT_P208 "CL1779252" @default.
- NCIT_C187042 NCIT_P322 "GDC" @default.
- NCIT_C187042 NCIT_P399 "809270" @default.
- NCIT_C187042 normalizedInformationContent "100" @default.
- NCIT_C187042 referenceCount "1" @default.
- NCIT_C187042 hasExactSynonym "BLU 451" @default.
- NCIT_C187042 hasExactSynonym "BLU-451" @default.
- NCIT_C187042 hasExactSynonym "EGFR Ex20ins Inhibitor BLU-451" @default.
- NCIT_C187042 hasExactSynonym "EGFR Exon 20 Insertion Inhibitor BLU-451" @default.
- NCIT_C187042 hasExactSynonym "EGFR Inhibitor BLU-451" @default.
- NCIT_C187042 hasExactSynonym "LNG 451" @default.
- NCIT_C187042 hasExactSynonym "LNG-451" @default.
- NCIT_C187042 hasExactSynonym "LNG451" @default.
- NCIT_C187042 inSubset NCIT_C128784 @default.
- NCIT_C187042 inSubset NCIT_C157711 @default.
- NCIT_C187042 inSubset NCIT_C157712 @default.
- NCIT_C187042 inSubset NCIT_C176424 @default.
- NCIT_C187042 type Class @default.
- NCIT_C187042 isDefinedBy ncit.owl @default.
- NCIT_C187042 label "EGFR Exon 20 Insertion Inhibitor BLU-451" @default.
- NCIT_C187042 subClassOf NCIT_C129824 @default.
- NCIT_C187042 subClassOf NCIT_C129825 @default.
- NCIT_C187042 subClassOf NCIT_C1404 @default.
- NCIT_C187042 subClassOf NCIT_C163758 @default.
- NCIT_C187042 subClassOf NCIT_C163952 @default.
- NCIT_C187042 subClassOf NCIT_C187042 @default.
- NCIT_C187042 subClassOf NCIT_C1908 @default.
- NCIT_C187042 subClassOf NCIT_C1909 @default.
- NCIT_C187042 subClassOf NCIT_C1967 @default.
- NCIT_C187042 subClassOf NCIT_C199379 @default.
- NCIT_C187042 subClassOf NCIT_C2167 @default.
- NCIT_C187042 subClassOf NCIT_C2189 @default.
- NCIT_C187042 subClassOf NCIT_C274 @default.
- NCIT_C187042 subClassOf NCIT_C471 @default.