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Ceritinib is an inhibitor of anaplastic lymphoma kinase (ALK, IC50 = 0.2 nM). 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. 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. 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.Formal Name: 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine. CAS Number: 1032900-25-6. Synonyms: LDK 378. Molecular Formula: C28H36ClN5O3S. Formula Weight: 558.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12 mg/mL, DMF:PBS(pH7.2) (1:2): 0.3 mg/mL, DMSO: 1 mg/mL, Ethanol: 16 mg/mL. lambdamax: 277, 303 nm. SMILES: CC(C=C(NC1=NC=C(Cl)C(NC2=CC=CC=C2S(C(C)C)(=O)=O)=N1)C(OC(C)C)=C3)=C3C4CCNCC4. InChi Code: InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34). InChi Key: VERWOWGGCGHDQE-UHFFFAOYSA-N.
Keywords:
LDK 378, 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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