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Bioluminescent imaging study FAK inhibitor, PF-562,271, preclinical study in PC3M-luc-C6 local implant and metastasis xenograft models

  1. Author:
    Sun, H. H.
    Pisle, S.
    Gardner, E. R.
    Figg, W. D.

  2. Author Address

    [Sun, Haihao; Figg, William D.] NCI, Mol Pharmacol Sect, Bethesda, MD 20892 USA. [Pisle, Stephen; Figg, William D.] NCI, Clin Pharmacol Program, Med Oncol Branch, Ctr Canc Res, Bethesda, MD 20892 USA. [Gardner, Erin R.] NCI Frederick, SAIC Frederick, Clin Pharmacol Program, Frederick, MD USA.;Figg, WD, NCI, Mol Pharmacol Sect, Bethesda, MD 20892 USA.;wdfigg@helix.nih.gov
    1. Year: 2010
    2. Date: Jul
  2. Journal: Cancer Biology & Therapy
    1. 10
    2. 1
    3. Pages: 38-43
  4. Type of Article: Article
  5. ISSN: 1538-4047
  1. Abstract:

    Focal adhesion kinase (FAK) is essential in regulating integrin signaling pathways responsible for cell survival and proliferation, as well as motility, making FAK a distinctive target in the field of anticancer drug development, especially with regards to metastatic disease.(1) Our objective was to demonstrate tumor growth inhibition by PF-562,271, a selective inhibitor of FAK and FAK2, or Pyk2,(2) in mouse xenograft models, both subcutaneous and metastatic, employing the human prostate cancer cell line PC3M-luc-C6, a modified PC3M cell line that expresses luciferase. After 2 weeks of treatment with PF-562,271, 25 mg/kg PO BID 5x/wk, the subcutaneous model showed a 62% tumor growth inhibition compared to control based on tumor measurements (p < 0.05), with a 88 vs. a 490% increase in bioluminescent signal for treatment and control respectively (p < 0.05). In the metastasis model, the percent change from baseline, after 18 days of treatment, of the treatment group was 2,854 vs. 14,190% for the vehicle (p < 0.01). These results show that PF-562,271 has a potent effect on metastatic prostate cancer growth in vivo.

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External Sources

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  2. DOI: 10.4161/cbt.10.1.11993
  3. View record in Web of Science®
  4. WOS: 000279593900007

Library Notes

  1. Fiscal Year: FY2009-2010
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