A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC50s = 0.2

AZD 4547 – 10 mg

Brand:
Cayman
CAS:
1035270-39-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.{24741} 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).{24741} AZD 4547 has demonstrated antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM).{24741} 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.{24741}  

 

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Description

A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC50s = 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively); demonstrates antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM) and in an FGFR-driven human tumor xenograft model (12.5 mg/kg/day)

Formal name: rel-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-benzamide

Synonyms: 

Molecular weight: 463.6

CAS: 1035270-39-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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