Crizotinib hydrochloride

Catalog No.S5190 Synonyms: Xalkori, PF-02341066 hydrochloride

For research use only.

Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.

Crizotinib hydrochloride Chemical Structure

CAS No. 1415560-69-8

Selleck's Crizotinib hydrochloride has been cited by 44 publications

Purity & Quality Control

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Biological Activity

Description Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Targets
ROS1 [2]
(Cell-free assay)
c-Met [1]
(Cell-based assay)
NPM-ALK [2]
(Cell-based assay)
<0.025 nM(Ki) 11 nM 24 nM

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 486.8
Formula

C21H23Cl3FN5O

CAS No. 1415560-69-8
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04148066 Recruiting Diagnostic Test: ctDNA blood sample Carcinoma Non-Small-Cell Lung The Netherlands Cancer Institute|Roche Pharma AG July 17 2019 Not Applicable
NCT03947385 Recruiting Drug: IDE196|Drug: Binimetinib|Drug: Crizotinib Metastatic Uveal Melanoma|Cutaneous Melanoma|Colorectal Cancer|Other Solid Tumors IDEAYA Biosciences June 28 2019 Phase 1|Phase 2
NCT03439215 Active not recruiting Drug: Lorlatinib Carcinoma Non-Small-Cell Lung Fondazione Ricerca Traslazionale|Clinical research technology Srl June 13 2017 Phase 2
NCT02946216 Unknown status Genetic: ctDNA analysis Non-small Cell Lung Cancer Stage III|Non-Small-Cell Lung Cancer Metastatic|Adenocarcinoma of Lung|EGFR Wildtype First People''s Hospital of Hangzhou November 2016 --
NCT02511184 Terminated Drug: Crizotinib|Drug: Pembrolizumab ALK-positive Advanced NSCLC Pfizer|Merck Sharp & Dohme Corp. October 2015 Phase 1
NCT02419287 Active not recruiting Drug: crizotinib Anaplastic Large Cell Lymphoma ALK-Positive University of Milano Bicocca April 2015 Phase 2

(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

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