Crizotinib (acetate)

• Description :

  Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate 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 acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition[1][2][3].

• Product Name Alternative :

  PF-02341066 (acetate)

• UNSPSC :

  12352005

• Target :

  Anaplastic lymphoma kinase (ALK) ; c-Met/HGFR; ROS Kinase

• Type :

  Reference compound

• Related Pathways :

  Protein Tyrosine Kinase/RTK

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/crizotinib-acetate.html

• Solubility :

  10 mM in DMSO

• Smiles :

  NC1=NC=C(C=C1O[C@H](C)C2=C(C=CC(F)=C2Cl)Cl)C3=CN(N=C3)C4CCNCC4.CC(O)=O

• Molecular Formula :

  C23H26Cl2FN5O3

• Molecular Weight :

  510.39

• References & Citations :

  [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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• CAS Number :

  [877399-53-6]