Crizotinib
Crizotinib is an inhibitor of anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), and c-MET, binding competitively to the ATP-binding pocket of kinases. Crizotinib exhibits anticancer chemotherapeutic benefit in the treatment of non-small cell lung cancer (NSCLC) and is currently in clinical trials as a potential treatment for neuroblastoma and other advanced solid tumors. In cellular models, this compound upregulates expression of pro-apoptotic BIM and downregulates expression of anti-apoptotic survivin to induce apoptosis and inhibit cell proliferation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18853944
| Cas No. |
877399-52-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C21H22Cl2FN5O |
| Formula Wt. |
450.34 |
| IUPAC Name |
3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine |
| Appearance |
White to off white powder |
Timm A, Kolesar JM. Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. PMID: 23686600.
Okamoto W, Okamoto I, Arao T, et al. Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. PMID: 22729845.
Tanizaki J, Okamoto I, Okamoto K, et al. MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations. J Thorac Oncol. 2011 Oct;6(10):1624-31. PMID: 21716144.
