Off target protein and potency:
KDR 24 nMFGFR4 165 nMIGFR 581 nMProbe Selectivity in Vitro:
Selectivity was examined against a diverse panel of representative human kinases and AZD4547 shown to inhibit recombinant VEGFR2 (KDR) kinase, No enzyme inhibition was detected against ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2, and PI3-kinase; FGFR4 cellular kinase activity (IC50 = 142 nmol/L). cellular KDR and IGFR ligand–induced phosphorylation (IC50 values of 258 and 828 nmol/L, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1.
