| 体内研究: |
EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC50s of 0.013 μM, 2.972 μM, 1.031 μM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively. EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM; 24 h) induces cell cycle attest at the G0/G1-phase. EGFR-IN-47 (0.01, 0.05, 0.25 μM) induces cell deathvia apoptosis in a concentration-dependent manner. EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM) inhibits phosphorylation of the EGFR downstream mediators. |