Ceritinib

Description: Ceritinib (LDK378) is an ALK tyrosine kinase inhibitor (IC50=200 pM) with selective, ATP-competitive, and oral activity. Ceritinib also inhibits IGF-1R, InsR, and STK22D (IC50=8/7/23 nM). Ceritinib has antitumor activity. Target: IGF-1R, Serine Protease, ALK. Smiles: N(C1=C(OC(C)C)C=C(C(C)=C1)C2CCNCC2)C=3N=C(NC4=C(S(C(C)C)(=O)=O)C=CC=C4)C(Cl)=CN3. References: Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25,56(14):5675-90.