(R)-Crizotinib-d5 is intended for use as an internal standard for the quantification of (R)-crizotinib by GC- or LC-MS. (R)-Crizotinib is a derivative of aminopyridine that acts as a potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC50 = 8 nM) and ALK (IC50 = 20 nM) receptor tyrosine kinases.1 (R)-Crizotinib shows antitumor efficacy, including cytoreductive antitumor activity, in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins (IC50s = 5-20 nM).1,2
1.Cui, J.J., Tran-DubÉ, M., Shen, H., 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.54(18)6342-6363(2011) 2.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 alterationsJ.Thorac.Oncol.6(10)1624-1631(2011)