AZD-4547

Описание

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. 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). AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC₅₀s = 18-281 nM). 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.

Химические свойства

Pale Yellow Solid

Использование

AZD4547 is a bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor (FGFR) tyrosine kinases. AZD4547 is particularly effective in inhibiting FGFR1, 2, and 3 tyrosine k inases and is under clinical investigation for the treatment of FGFR-dependent tumors.