Ceritinib dihydrochloride

Catalog No.S4967 Synonyms: Zykadia, LDK378 dihydrochloride

For research use only.

Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity.

Ceritinib dihydrochloride Chemical Structure

CAS No. 1380575-43-8

Selleck's Ceritinib dihydrochloride has been cited by 9 Publications

Purity & Quality Control

Choose Selective ALK Inhibitors

Other ALK Products

Biological Activity

Description Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity.
Targets
ALK [1]
(Cell-free assay)
InsR [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
STK22D [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM 23 nM

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 13 mg/mL
(20.6 mM)
Water Insoluble
Ethanol '''10 mg/mL

Chemical Information

Molecular Weight 631.06
Formula

C28H38Cl3N5O3S

CAS No. 1380575-43-8
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03087448 Recruiting Drug: Ceritinib|Drug: Trametinib Non-small Cell Lung Cancer University of California San Francisco|Novartis Pharmaceuticals|University of California Davis September 9 2017 Phase 1|Phase 2
NCT02638909 Terminated Drug: ceritinib Colorectal Adenocarcinoma|Cholangiocarcinoma|Pancreatic Adenocarcinoma|Hepatocellular Adenocarcinoma|Gastric Adenocarcinoma|Esophageal Adenocarcinoma Criterium Inc.|University of Colorado Denver|Novartis December 2015 Phase 2
NCT02422589 Completed Drug: ceritinib|Drug: warfarin|Drug: midazolam ALK-positive Advanced Tumors Novartis Pharmaceuticals|Novartis October 23 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ceritinib dihydrochloride | Ceritinib dihydrochloride supplier | purchase Ceritinib dihydrochloride | Ceritinib dihydrochloride cost | Ceritinib dihydrochloride manufacturer | order Ceritinib dihydrochloride | Ceritinib dihydrochloride distributor