ASP3026

ASP3026 is a potent ALK (Anaplastic Lymphoma Kinase) inhibitor. ASP3026 inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel. In an anchorage independent in vitro cell growth assay, ASP3026 inhibited the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3 and that of 3T3 cells expressing EML4-ALK variant 1, 2 and 3. The plasma and tumor concentrations of ASP3026 in mice xenografted with NCI-H2228 tumor were determined using high-performance liquid chromatography-tandem mass spectrometry. ASP3026 showed potent anti-tumor effects while crizotinib was ineffective even at 100 mg/gk qd in an EML4-ALK driven tumor model with gatekeeper mutation.