Altiratinib is a multiple kinase inhibitor, blocking Met, Tie2, VEGF2, TrkA, TrkB, and TrkC with IC50 values of 2.7, 8.0, 9.2, 0.85, 4.6, and 0.83 nM, respectively. It also inhibits several mutant Met isoforms at nanomolar concentrations. Altiratinib inhibits the proliferation of several cancer cell lines in vitro and blocks capillary tube formation by HMVEC cells. It is orally bioavailable and penetrates the blood brain barrier, suppressing the growth of subcutaneous and intracerebroventricular xenograft tumors in mice.