Chemical Name: rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
Biological ActivityAZD 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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