Crizotinib hydrochloride

For research use only.

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

28 publications

Crizotinib hydrochloride Chemical Structure

CAS No. 1415560-69-8

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.

Selleck's Crizotinib hydrochloride has been cited by 28 publications

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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

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.26 mM)
Water 97 mg/mL (199.26 mM)
Ethanol ''97 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 486.8
Formula

C21H23Cl3FN5O

CAS No. 1415560-69-8
Storage powder
in solvent
Synonyms Xalkori, PF-02341066 hydrochloride

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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

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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID