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Biological Activity:
Potent, selective and ATP-competitive inhibitor of c-Met/HGF receptor and the nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), with IC50 values to be 4 and 25 nM for C-Met and ALK resepectively.
References: online 1 2 3 4
HY Zou 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, 4408. [online]
SH Ou et al. Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification. J. Thor. Oncol. 2011, 6(5), 942-946. [online]
U McDermott et al. Genomic Alterations of Anaplastic Lymphoma Kinase May Sensitize Tumors to Anaplastic Lymphoma Kinase Inhibitors. Cancer Res. 2008, 68(9), 3389-3395. [online]
Chemical Name: (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
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