ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

Mice harboring subcutaneous NCI-H2228 tumor xenografts were treated twice daily with the oral administration of ASP3026 for 14 days, which induced a dose-dependent antitumor effect, starting at 1 mg/kg and showing a pronounced reduction at 10, 30, and 100 mg/kg.

ASP3026 inhibits the growth of the NCI-H2228 human NSCLC tumor cell line, which endogenously expresses the EML4-ALK variant 3, with an IC50 value of 64.8 nM. ASP3026 demonstrates enhanced selectivity in inhibiting ALK activity in tyrosine kinases compared to PF02341066.

Recombinant truncated FLAG-tagged mTOR expressed in HEK 293 cells is used in biochemical assays, together with a biotinylated p70S6K peptide substrate. Streptavidin donor and protein A acceptor beads are used to assemble the capture complex for generation of the assay signal. The activity of the lipid kinases, PI3K alpha, beta, delta, and gamma are measured using recombinant proteins and the lipid PIP2 as substrate. Assays for ATM and DNA-PK activity are performed. The mTOR cellular activity is measured in MDAMB468 cells, using an Acumen laser scanning cytometer to analyze the levels of phosphorylation of S6 (Ser235/236) and AKT (Ser473)[1].