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Molecular properties generated using the CDK
|Compound class||Synthetic organic|
|International Nonproprietary Names|
|compound 47 [PMID: 27433829] | EGF-816 | EGF816|
|EGF816 is an irreversible and selective inhibitor of EGFRs harbouring gatekeeper T790M, and sensitising L858R mutations, whilst sparing the wild-type receptor (such compounds are termed third generation EGFR tyrosine kinase inhibitors) . It has been developed to overcome acquired resistance to, and side-effect liabilities of first and second generation EGFR inhibitors in non-small-cell lung cancer (NSCLC). Small-molecule EGFR T790M inhibitors and the development of novel compounds in the discovery pipeline are reviewed by Song et al. (2016) .
EGF816 is claimed in Novartis' patent WO2015085482 , where it is named (R,E)-N-(7-chloro-l-(l-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-lH-benzo[d]imidazol-2-yl)-2-methylisonicotinamide, which resolves to the IUPAC name presented here.
Preclinical characterisation is reported in .
|GtoPdb PubChem SID||315661280|
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|Search PubMed clinical trials||nazartinib|
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