App Note

Inhibition of FGFR signaling pathways studied in cancer cell lines using HTRF®

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Study of FGFR signaling pathway inhibition with HTRF technology

FGFR genetic alterations have been reported in a wide variety of cancers, including breast, lung, ovarian, gastric, and prostate tumors. The tyrosine kinase receptors, once phosphorylated, activate different signaling pathways (RAS-MAPK, PI3K-AKT, PLCγ, and STAT) that act on cell proliferation, survival, migration, and adhesion or differentiation. Altogether, this makes FGFRs prime targets for tyrosine kinase inhibitors in anticancer strategies.

In this application note, the inhibitor AZD4547, currently in clinical trials and capable of inhibiting or suppressing the abnormal phosphorylation of FGFRs, was used in three different types of cancer cell lines: KG-1, SNU-16, and KMS-11. Its effects were detected using HTRF technology. The assays represent a fast, reliable, and sensitive method for quantifying total protein and phosphoprotein expression levels to monitor cell signal transduction in these different cell lines.

In this application note, you will learn more about the:

  • Study of the activation state of FGFR receptors and downstream effectors to deconvolute pathways in various cell cancer models
  • Measurement of the level of expression of total proteins and phosphoproteins (FGFR, ERK, PLCG1, STAT5, MEK…)
  • Measurements of the inhibitor’s effectiveness and comparison of the IC50 obtained with data reported in the literature.

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