产品描述:
AZD 4547 is a selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinase with IC50 values of 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively.{24741} It displays weaker activity against FGFR4 (IC50 = 165 nM), VEGFR2 (IC50 = 24 nM), and a panel of other tyrosine and serine/theronine kinases such as insulin-like growth factor 1 receptor (IC50 = 581 nM), cyclin-dependent kinase 2 (IC50 = >10 μM), and p38 (IC50 = >100 μM).{24741} AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM).{24741} In an FGFR-driven human tumor xenograft mouse model, oral administration of AZD 4547 at concentrations up to 12.5 mg/kg/day resulted in potent dose-dependent antitumor activity.{24741}