An orally active ALK inhibitor
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.1 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.1 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.1
1.Chang, M., Quail, M.R., Gingrich, D.E., et al.CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancersMol. Cancer Ther.11(3)670-679(2012)
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