1. Academic Validation
  2. The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer

The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer

  • Oncogenesis. 2018 Sep 20;7(9):73. doi: 10.1038/s41389-018-0083-1.
Stefanie Tiede 1 Nathalie Meyer-Schaller 1 Ravi Kiran Reddy Kalathur 1 2 Robert Ivanek 1 2 Ernesta Fagiani 1 Philip Schmassmann 1 Patrick Stillhard 1 Simon Häfliger 1 Norbert Kraut 3 Norbert Schweifer 3 Irene C Waizenegger 3 Ruben Bill 4 Gerhard Christofori 5
Affiliations

Affiliations

  • 1 Department of Biomedicine, University of Basel, 4058, Basel, Switzerland.
  • 2 Swiss Institute of Bioinformatics, 4053, Basel, Switzerland.
  • 3 Boehringer Ingelheim RCV GmbH & Co KG, 1121, Vienna, Austria.
  • 4 Department of Biomedicine, University of Basel, 4058, Basel, Switzerland. rubenmichael.bill@insel.ch.
  • 5 Department of Biomedicine, University of Basel, 4058, Basel, Switzerland. gerhard.christofori@unibas.ch.
Abstract

Focal adhesion kinase (FAK) is a cytoplasmic tyrosine kinase that regulates a plethora of downstream signaling pathways essential for cell migration, proliferation and death, processes that are exploited by Cancer cells during malignant progression. These well-established tumorigenic activities, together with its high expression and activity in different Cancer types, highlight FAK as an attractive target for Cancer therapy. We have assessed and characterized the therapeutic potential and the biological effects of BI 853520, a novel small chemical inhibitor of FAK, in several preclinical mouse models of breast Cancer. Treatment with BI 853520 elicits a significant reduction in primary tumor growth caused by an anti-proliferative activity by BI 853520. In contrast, BI 853520 exerts effects with varying degrees of robustness on the different stages of the metastatic cascade. Together, the data demonstrate that the repression of FAK activity by the specific FAK Inhibitor BI 853520 offers a promising anti-proliferative approach for Cancer therapy.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-122844
    99.86%, FAK抑制剂
    FAK