Ceritinib (LDK-378; Zykadia)

Description: Ceritinib (formerly known as LDK378; trade name: Zykadia) is novel, potent and selective inhibitor against ALK (anaplastic lymphoma kinase positive) with potential anticancer activity. It inhibits ALK with IC50 of 0.2 nM in cell-free assays, and shows 40- and 35-fold selectivity for ALK over IGF-1R and InsR, respectively. Ceritinib was approved by FDA in April 2014 for the treatment non-small cell lung cancer (NSCLC). In Phase I trials, Ceritinib showed a marked clinical response in 78 patients with anaplastic ALK+ metastatic non-small cell lung cancer who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib.

References: J Med Chem. 2013 Jul 25; 56(14):5675-90.

Related CAS: 1380575-43-8 (2HCl); 1032900-25-6 (free base); 1190399-48-4 (x-HCl);

LDK 378; Ceritinib; LDK378; LDK-378; trade name: Zykadia.

Chemical Name: 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2, 4-diamine

Exact Mass: 557.22274