Ceritinib, Free Base (LDK-378, Zykadia, CAS 1032900-25-6), >99%

LC Laboratories' Product Number C-2086 - Ceritinib, Free Base (LDK-378, Zykadia, CAS 1032900-25-6), >99% - for research use only. Ceritinib, also known as LDK-378, is a very selective anaplastic lymphoma kinase (ALK) inhibitor. It inhibits ALK with an IC50 of 200 pM. It inhibits kinases IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively and other kinases tested with IC50s of >100 nM. In vivo it displayed efficacy in anaplastic large cell lymphoma (ALCL) and non-small-cell lung cancer (NSCLC) cancer xenograft models at well-tolerated doses. Non-small-cell lung cancers (NSCLC) harboring ALK gene rearrangements always develop resistance to the ALK tyrosine kinase inhibitor crizotinib. Ceritinib effectively inhibited crizotinib-resistant ALK with L1196M, G1269A, I1171T and S1206Y mutations. However, ceritinib did not overcome two crizotinib-resistant ALK mutations, G1202R and F1174C. A phase 1 clinical trial showed ceritinib was highly active in patients with advanced, ALK-rearranged NSCLC. Certinib was also active in patients who had had disease progression during crizotinib treatment regardless of the presence of resistance mutations in ALK. Ceritinib is the active ingredient in the drug product sold under the trade name Zykadia®. This drug is currently approved in at least one country for use in patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) following treatment with crizotinib. NOTE: THE CERITINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT ZYKADIA®, AND IS NOT FOR HUMAN USE. Related CAS numbers: 1380575-43-8 for the dihydrochloride salt. Another CAS number previously assigned to Ceritinib free base, namely 1431456-10-8, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: C-2086
• Sku #: C-2086_1g