Ontology highlight
ABSTRACT:
SUBMITTER: Zhang Z
PROVIDER: S-EPMC5911580 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Cancer medicine 20180313 4
YL143 was identified as a novel wild-type sparing EGFR<sup>T790M</sup> inhibitor with good pharmacokinetic properties. It potently suppresses EGFR<sup>L858R/T790M</sup> with an 50% inhibitory concentration (IC<sub>50</sub> ) value of 2.0 ± 0.3 nmol/L, but is approximately 92-folds less potent against EGFR<sup>WT</sup> kinase. YL143 suppresses cellular proliferation and induces G0/G1 phase arrest and apoptosis in H1975 cells with EGFR<sup>L858R/T790M</sup> mutation at 30 nmol/L. It also exhibits ...[more]