Description
AZD4547 can potently and selectively inhibit FGFR1, FGFR2 and FGFR3 with IC50 of 0.2 nM, 2.5 nM and 1.8 nM.
Storage
2 years at -20centigrade Powder
Targets
FGFR1, FGFR2, FGFR3
Molecular Formula
C26H33N5O3
Chemical Name
N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide
Solubility
DMSO 92 mg/mL Water
In vitro
As a inhibitor of the fibroblast growth factor receptor tyrosine kinase family, AZD4547 can potently and selectively inhibit FGFR1, FGFR2 and FGFR3. AZD4547 is different other FGFR inhibitor, which is against the kinase insert domain receptor (KDR). AZD4547 inhibited recombinant FGFR kinase activity in vitro and suppressed FGFR signaling and growth in tumor cell lines with deregulated FGFR expression.
In vivo
In a representative FGFR-driven human tumor xenograft model, oral administration of AZD4547 was well tolerated and resulted in potent dose-dependent antitumor activity. At efficacious doses, no evidence of anti-KDR-related effects were observed, confirming the in vivo FGFR selectivity of AZD4547.
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