1. Protein Tyrosine Kinase/RTK
  2. ALK
    Insulin Receptor
    IGF-1R
  3. Ceritinib dihydrochloride

Ceritinib dihydrochloride (Synonyms: LDK378 dihydrochloride)

Cat. No.: HY-15656A Purity: 99.98%
Handling Instructions

Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.

For research use only. We do not sell to patients.

Ceritinib dihydrochloride Chemical Structure

Ceritinib dihydrochloride Chemical Structure

CAS No. : 1380575-43-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 69 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Ceritinib dihydrochloride:

Top Publications Citing Use of Products

    Ceritinib dihydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006.

    Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.
    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency[1][2].

    IC50 & Target

    IC50: 0.2 nM (ALK), 8 nM (IGF-1R), 7 nM (InsR), 23 nM (STK22D)[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].

    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].

    Clinical Trial
    Molecular Weight

    631.06

    Formula

    C₂₈H₃₈Cl₃N₅O₃S

    CAS No.

    1380575-43-8

    SMILES

    CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 170 mg/mL (269.39 mM)

    DMSO : 100 mg/mL (158.46 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5846 mL 7.9232 mL 15.8464 mL
    5 mM 0.3169 mL 1.5846 mL 3.1693 mL
    10 mM 0.1585 mL 0.7923 mL 1.5846 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (3.96 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    CeritinibLDK378LDK 378LDK-378ALKInsulin ReceptorIGF-1RAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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    Product name:
    Ceritinib dihydrochloride
    Cat. No.:
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