Anaplastic lymphoma kinase (ALK) is really a tyrosine kinase that’s constitutively activated in a few cancers, following gene alterations for example genetic translocation, amplification, or point mutation. Here, we identified CH5424802, a powerful, selective, and orally available ALK inhibitor having a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, for example nonsmall cell cancer of the lung (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro as well as in vivo. CH5424802 inhibited ALK L1196M, which matches the gatekeeper mutation conferring common potential to deal with kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Our results support the opportunity of clinical look at CH5424802 to treat patients with ALK-driven tumors.