Cancer of the lung may be the leading reason for cancer mortality on the planet. Even though some advances in cancer of the lung therapy happen to be made, patient survival continues to be poor. The platelet-derived growth factor receptors (PDGFRs) as well as their ligands play critical roles within the regulating many cancer cell processes, including cell survival and cell motility. Herein, we investigate anticancer activities of CP-673451, a powerful selective inhibitor of PDGFR kinase, in non-small-cell cancer of the lung (NSCLC) therapy. We discovered that Clubpenguin-673451 works well at suppressing cell viability, inducing cell apoptosis, and inhibiting cell migration and invasion by suppressing the PDGFR downstream signaling path in NSCLC cells. In addition, CP-673451 works well at suppressing NSCLC tumor development in vivo. In conclusion, our studies claim that CP-673451 may well be a promising therapeutic compound for NSCLC.