Sunday, December 21, 2014


Common name: Crizotinib; PF-02341066; PF02341066; Xalkori
Trademarks:  Xalkori
Molecular Formula: C21H22Cl2FN5O
CAS Registry Number: 877399-52-5
CAS Name: 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
Molecular Weight: 450.337
Activity: Oncolytic Drugs; Protein Kinase Inhibitor; Anaplastic Lymphoma Kinase Inhibitor; Lung Cancer Drug; ALK Inhibitor

Crizotinib synthesis: Org Process Res Dev 2011, 15, 1018-1026

1. Cui, J. J.; et. al. Crizotinib, a c-Met protein kinase inhibitor anticancer agent; 3-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine is crizotinib. US7858643B2
2. Cui, J. J.; et. al. Aminoheteroaryl compounds as protein kinase inhibitors. WO2004076412A2
3. De Koning, P. D.; et. al. Fit-for-Purpose Development of the Enabling Route to Crizotinib (PF-02341066). Org Process Res Dev 2011, 15(5), 1018-1026.
4. Cui, J. J.; 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, 54(18), 6342-6363.