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    Ceritinib (LDK-378; Zykadia)
    Ceritinib (LDK-378; Zykadia)

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    数量: - + 件(库存件)
    InvivoChem目录号 #: V0154
    CAS号码 #: 1032900-25-6 纯度 ≥98%

    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);

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    Molecular Weight (MW)558.14
    FormulaC28H36ClN5O3S
    CAS No.1032900-25-6 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (35.8 mM)          
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (5.4 mM)
    SMILESClC1=CN=C(NC2=CC(C)=C(C3CCNCC3)C=C2OC(C)C)N=C1NC4=CC=CC=C4S(C(C)C)(=O)=O
    Synonyms

    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 


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    In Vitro

    In vitro activity: Ceritinib (formerly known as LDK378; trade name: Zykadia) is novel, potent and selective inhibitor against ALK (anaplastic lymphoma kinase positive) with IC50 of 0.2 nM in cell-free assays, it shows 40- and 35-fold selectivity against 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.  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.


    Kinase Assay: All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement).


    Cell Assay: Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.

    In VivoLDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. 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. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.
    Animal modelRNU nude rats bearing the Karpas299/H2228 tumors
    Formulation & DosageFormulated in 0.5% methylcellulose/0.5% Tween 80;  50 mg/kg;  Oral gavage
    ReferencesJ Med Chem. 2013 Jul 25;56(14):5675-90.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Ceritinib (LDK378)

    Dose–response and time course comparison of ALK inhibition by crizotinib or ceritinib.  2017 Aug;11(8):996-1006.

    Ceritinib (LDK378)

    Tumor volume measurement and MSD ® immunoassay quantitation of Th‐ALKF 1174L/MYCNtumors following the treatment with crizotinib or ceritinib. Tumor‐bearing animals were treated with either crizotinib (100 mg·kg−1 per day, orally) or ceritinib (100 mg·kg−1 per day, orally) for 7 days before animal sacrifice and harvesting of tumor tissue samples.

    Ceritinib (LDK378)

    Basal ALK activity in neuroblastoma cell lines. (A) Immunoblots of lysates from neuroblastoma cell line panel, including lysate from Ba/F3 ALK F1174L as a positive control for ALK expression and lysate from Hela cells as negative control for ALK expression.  2017 Aug;11(8):996-1006.


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