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HomeProduct name listAZD-4547

AZD-4547

AZD-4547 Structural

What is AZD-4547?

Description

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.

Chemical properties

Pale Yellow Solid

The Uses of AZD-4547

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.

Definition

ChEBI: AZD4547 is a member of the class of benzamides that is a carboxamide resulting from the formal condensation of the carboxy group of 4-(cis-3,5-dimethylpiperazin-1-yl)benzoic acid with the amino substituent of 5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-amine. It is an inhibitor of the fibroblast growth factor receptor (FGFR). It has a role as a fibroblast growth factor receptor antagonist. It is a member of pyrazoles, a N-arylpiperazine and a member of benzamides.

What are the applications of Application

AZD4547 is a novel selective FGFR inhibitor targeting Flg (FGFR1), Bek (FGFR2), and FGFR-3

storage

Store at -20°C

Properties of AZD-4547

Melting point: 168-170°C
Boiling point: 621.7±55.0 °C(Predicted)
Density  1.189
storage temp.  Refrigerator
solubility  DMSO (Slightly), Methanol (Slightly)
form  Solid
pka 13.66±0.10(Predicted)
color  Pale Yellow to Light Beige

Safety information for AZD-4547

Computed Descriptors for AZD-4547

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