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Application Note

No-Wash IP1 assays are a powerful readout to characterize compounds modulating the FGFR signaling pathway in cancer drug research

The success of cancer therapies can be influenced by the interaction between multiple signaling pathways. Dysregulated FGFR signaling has been found in various types of cancer. The complexity and multitude of FGFR intracellular signaling pathways necessitate the development of specific investigational tools to better understand a drug’s mechanism of action.

D-myo-Inositol 1-Phosphate (IP1), an intracellular metabolite of IP3, has been widely used in cell-based high-throughput assays for GPCR agonist and antagonist screening as a surrogate biomarker for IP3. This application note demonstrates that detecting the intracellular accumulation of IP1, mediated by FGFR-dependent activation of PLCγ1, can be a powerful alternative for characterizing compounds that modulate FGFR signaling in various cancer cell lines expressing FGFR1, FGFR2, and FGFR3.

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  • detailed pathways
  • description of assay principles
  • materials and methods, results and discussion about this study

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No-Wash IP1 assays are a powerful readout to characterize compounds modulating the FGFR signaling pathway in cancer drug research

Download Application Note