AZD 4547

Biological Activity

AZD 4547 is a potent and selective FGFR1, FGFR3 and FGFR2 tyrosine kinase inhibitor (IC₅₀ values are 0.2 1.8, and 2.5 nM, respectively). It shows selectivity for FGFR across a range of unrelated tyrosine and serine/threonine kinases, including IGFR (>2,900-fold), CDK2 (>50,000-fold), and p38 (>50,000-fold). In vitro, it has antiproliferative effects on tumor cell lines with deregulated FGFR expression. In vivo, AZD 4547 exhibits dose-dependent inhibition of tumor growth in an FGFR-driven human tumor xenograft mice model. It suppresses osteoclastogenesis and tumor-induced osteolysis in an orthotopic breast cancer bone metastasis mouse model. AZD 4547 is orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family.
   Gavine PR, Mooney L, Kilgour E
   Cancer Res., 2012;72(8):2045-56.

Product Datasheets