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Product 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].
Web ID
– HY-50878B
Shipping
– Room temperature
Molecular Formula
– C23H26Cl2FN5O3
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]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.|[3]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.
CAS Number
– 877399-53-6
Molecular Weight
– 510.39
SMILES
– NC1=NC=C(C=C1O[C@H](C)C2=C(C=CC(F)=C2Cl)Cl)C3=CN(N=C3)C4CCNCC4.CC(O)=O
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Anaplastic lymphoma kinase (ALK);c-Met/HGFR;ROS Kinase
Pathway
– Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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