1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
    Insulin Receptor
    IGF-1R
  3. Ceritinib dihydrochloride

Ceritinib dihydrochloride  (Synonyms: LDK378 dihydrochloride)

Cat. No.: HY-15656A Purity: 99.83%
COA 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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 76 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 76 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 77 In-stock
Estimated Time of Arrival: December 31
50 mg USD 110 In-stock
Estimated Time of Arrival: December 31
100 mg USD 165 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 24 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.  [Abstract]

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

    • Purity & Documentation

    • References

    • 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    631.06

    Formula

    C28H38Cl3N5O3S

    CAS No.
    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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

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

    H2O : 10 mg/mL (15.85 mM; Need ultrasonic)

    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:  PBS

      Solubility: 100 mg/mL (158.46 mM); Clear solution; Need ultrasonic

    • 2.

      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

    • 3.

      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

    • 4.

      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 available by MCE.
    Purity & Documentation

    Purity: 99.83%

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Ceritinib dihydrochloride
    Cat. No.:
    HY-15656A
    Quantity:
    MCE Japan Authorized Agent: