Structure-Activity Relationship of Indole-Tethered Pyrimidine Derivatives that Concurrently Inhibit Epidermal Growth Factor Receptor and Other Angiokinases
Fig 3
MKP101 inhibits proliferation of epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-sensitive non-small cell lung cancer (NSCLC) cells.
(A) Inhibition of HCC827 cell proliferation. Cells were incubated for 72 h with a range of concentrations of MKP101, and cell viability was measured using the WST-1 assay. The IC50 value was 160 nM. (B) Inhibition of EGFR phosphorylation in HCC827 cells. Western blot analysis using antibodies to phosphorylated and total EGFR from a representative experiment is shown. Cells were incubated for 3 h at the indicated concentration. (C) Graph showing the relative intensities of the total and phosphorylated EGFR as determined by band densitometry. IC50, half-maximal inhibitory concentration.