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LDK-378 dihydrochloride(Ceritinib dihydrochloride)

  Cat. No.:  DC31186   Featured
Chemical Structure
1380575-43-8
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Field of application
Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1380575-43-8
Chemical Name: LDK378 2Hcl (Ceritinib)
Synonyms: LDK378 2Hcl (Ceritinib);5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine,dihydrochloride;LDK-378-2HCl salt;Ceritinib dihydrochloride;LDK 378 dihydrochloride;LDK-378 dihydrochloride
SMILES: Cl.Cl.CC1=C(C2CCNCC2)C=C(OC(C)C)C(NC2=NC=C(Cl)C(NC3=C(S(C(C)C)(=O)=O)C=CC=C3)=N2)=C1
Formula: C28H38Cl3N5O3S
M.Wt: 631.057022571564
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ceritinib dihydrochloride (LDK378 dihydrochloride) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
Target: IC50: 0.2 nM (ALK)[1].
In Vivo: Ceritinib (LDK378) is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. Ceritinib (LDK378) has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. Ceritinib (LDK378) exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. Ceritinib (LDK378) induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. Ceritinib (LDK378) shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg[1].
In Vitro: Ceritinib (LDK378) shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells[1].
References: [1]. 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, Jun 6.
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