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Article

YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFRL858R, T790M -mutant resistance in vitro and in vivo.

Cancer medicine - 1 Apr 2018

Zhang Zhang, Zou Jian, Yu Lei, Luo Jinfeng, Li Yan, Tu Zhengchao, Ren Xiaomei, Wei Hongcheng, Song Liyan, Lu Xiaoyun, Ding Ke

Abstract excerpt

YL143 was identified as a novel wild-type sparing EGFRT790M inhibitor with good pharmacokinetic properties. It potently suppresses EGFRL858R/T790M with an 50% inhibitory concentration (IC50 ) value of 2.0 ± 0.3 nmol/L, but is approximately 92-folds less potent against EGFRWT kinase. YL143 suppresses cellular proliferation and induces G0/G1 phase arrest and apoptosis in H1975 cells with EGFRL858R/T790M mutation at...

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Identifiers

PMID: 29532998
DOI: 10.1002/cam4.1392
PMCID: PMC5911580

Genes

EGFR

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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