Crizotinib acetate

Names

[ CAS No. ]:
877399-53-6

[ Name ]:
Crizotinib acetate

[Synonym ]:
Crizotinib acetate

Biological Activity

[Description]:

Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ROS
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[References]

[1]. Zou HY, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007, 67(9), 4408-4417.  

[2]. Christensen JG, et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322.  

[3]. Cui JJ, et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63.  

Chemical & Physical Properties

[ Molecular Formula ]:
C23H26Cl2FN5O3

[ Molecular Weight ]:
510.38900

[ Exact Mass ]:
509.14000

[ PSA ]:
115.29000

[ LogP ]:
6.03860

Related Compounds