CEP-28122 is a potent inhibitor of anaplastic lymphoma kinase (ALK; IC50 = 1.9 nM) that less potently inhibits other tyrosine and serine/threonine kinases. It blocks the phosphorylation of ALK and other ALK substrates in cells and induces concentration-dependent growth inhibition or cytotoxicity of ALK-positive cancer cells. CEP-28122 is orally active, inhibiting ALK tyrosine phosphorylation in tumor xenografts in mice for more than 12 hours following single oral dosing at 30 mg/kg.
