YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR(L858R, T790M)‐mutant resistance in vitro and in vivo

YL143 was identified as a novel wild‐type sparing EGFR(T790M) inhibitor with good pharmacokinetic properties. It potently suppresses EGFR(L858R/T790M) with an 50% inhibitory concentration (IC(50)) value of 2.0 ± 0.3 nmol/L, but is approximately 92‐folds less potent against EGFR(WT) kinase. YL143 sup...

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Publicado en:Cancer Med
Autores principales: Zhang, Zhang, Zou, Jian, Yu, Lei, Luo, Jinfeng, Li, Yan, Tu, Zhengchao, Ren, Xiaomei, Wei, Hongcheng, Song, Liyan, Lu, Xiaoyun, Ding, Ke
Formato: Artigo
Lenguaje:Inglês
Publicado: John Wiley and Sons Inc. 2018
Materias:
Cancer Prevention
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC5911580/
https://ncbi.nlm.nih.gov/pubmed/29532998
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cam4.1392
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