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Submit ReviewAZD 4547
Description: Potent and selective FGFR inhibitor
Chemical Name: rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
Purity: ≥98% (HPLC)
Biological Activity for AZD 4547
AZD 4547 is a potent and selective FGFR1, FGFR3 and FGFR2 tyrosine kinase inhibitor (IC50 values are 0.2 1.8, and 2.5 nM, respectively). It shows selectivity for FGFR across a range of unrelated tyrosine and serine/threonine kinases, including IGFR (>2,900-fold), CDK2 (>50,000-fold), and p38 (>50,000-fold). In vitro, it has antiproliferative effects on tumor cell lines with deregulated FGFR expression. In vivo, AZD 4547 exhibits dose-dependent inhibition of tumor growth in an FGFR-driven human tumor xenograft mice model. It suppresses osteoclastogenesis and tumor-induced osteolysis in an orthotopic breast cancer bone metastasis mouse model. AZD 4547 is orally bioavailable.
Technical Data for AZD 4547
| M. Wt | 463.56 |
| Formula | C26H33N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1035270-39-3 |
| PubChem ID | 51039095 |
| InChI Key | VRQMAABPASPXMW-HDICACEKSA-N |
| Smiles | C[C@H]1CN(C2=CC=C(C=C2)C(NC3=NNC(CCC4=CC(OC)=CC(OC)=C4)=C3)=O)C[C@H](N1)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZD 4547
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.27 | 20 |
Preparing Stock Solutions for AZD 4547
The following data is based on the product molecular weight 463.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 10.79 mL | 53.93 mL | 107.86 mL |
| 1 mM | 2.16 mL | 10.79 mL | 21.57 mL |
| 2 mM | 1.08 mL | 5.39 mL | 10.79 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
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Product Datasheets for AZD 4547
References for AZD 4547
References are publications that support the biological activity of the product.
Gavine et al (2012) AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 72 2045 PMID: 22369928
Kang et al (2019) A selective FGFR inhibitor AZD4547 suppresses RANKL/M-CSF/OPG-dependent ostoclastogenesis and breast cancer growth in the metastatic bone microenvironment. Sci.Rep. 9 8726 PMID: 31217507
If you know of a relevant reference for AZD 4547, please let us know.
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Keywords: AZD 4547, AZD 4547 supplier, AZD4547, potent, selective, tyrosine, kinases, inhibitors, inhibits, FGFR, orally, bioavailable, osteolysis, cancer, osteoclastogenesis, 7823, Tocris Bioscience
Citations for AZD 4547
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