Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-[1-(methyl-d3)ethoxy-1,2,2,2-d4]-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine
Purity: ≥99% deuterated forms (d1-d7)
Formula Markup: C28H29D7ClN5O3S
Formula Weight: 565.17846
CAS Number: 1632484-77-5
Notes: Ceritinib-d7 is intended for use as an internal standard for the quantification of ceritinib (Item No. 19374) by GC- or LC-MS. Ceritinib is an inhibitor of anaplastic lymphoma kinase (ALK; IC50 = 0.2 nM).{48716} It is selective for ALK over IGF-1R, InsR, STK22D, and FLT3 (IC50s = 8, 7, 23, and 60 nM, respectively) as well as a panel of 25 additional kinases (IC50s = >0.26 μM for all). Ceritinib inhibits the proliferation of Ba/F3 cells expressing the fusion protein nucleophosmin-ALK (NPM-ALK) or echinoderm microtubule-associated protein-like 4-ALK (ELM4-ALK; IC50s = 0.02 and 0.021 μM, respectively), as well as several crizotinib-resistant NPM-ALK and ELM4-ALK mutants.{31295} It reduces tumor growth in an H2228 non-small cell lung cancer (NSCLC) rat xenograft model when administered at a dose of 10 mg/kg per day and induces tumor regression at 25 mg/kg per day.{48716} Ceritinib (25 and 50 mg/kg per day) also induces tumor regression in a Karpas299 lymphoma rat xenograft model. Formulations containing ceritinib have been used in the treatment of ALK-positive metastatic NSCLC.
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