AZD4547 is a pyrazole-based, FGFR1, FGFR2, and FGFR3 inhibitor with IC50 potency of 0.2, 2.5, and 1.8 nM, respectively. Besides modest activity against KDR (IC50, 24 nM), AZD4547 displays high selectivity towards unrelated tyrosine and serine-threonine kinases. [1] In cells, AZD4547 inhibits autophosphorylation of FGFR1, 2, and 3 at IC50 values of 12, 2, and 40 nM, respectively, along with downstream components, MAPK, FRS2, and PLCg in a dose-dependent manner. Antiproliferative effects of AZD4547 were observed predominantly in tumor cell lines with deregulated FGFR expression.

Preclinical studies indicate that AZD4547 does not induce known deleterious effects normally associated and characterized with KDR inhibition.