Ceritinib dihydrochloride

For research use only.

Catalog No.S4967 Synonyms: Zykadia, LDK378 dihydrochloride

6 publications

Ceritinib dihydrochloride Chemical Structure

CAS No. 1380575-43-8

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.

Selleck's Ceritinib dihydrochloride has been cited by 6 publications

Purity & Quality Control

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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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 631.06
Formula

C28H38Cl3N5O3S

CAS No. 1380575-43-8
Storage powder
in solvent
Synonyms Zykadia, LDK378 dihydrochloride

In vivo Formulation Calculator (Clear solution)

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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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

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

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID