All AbMole products are for research use only, cannot be used for human consumption.
AZD4547 (Fexagratinib) is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.
Inflammation. 2019 Dec;42(6):1957-1967.
Inhibition of Fibroblast Growth Factor Receptor by AZD4547 Protects Against Inflammation in Septic Mice.
AZD4547 purchased from AbMole
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Source | Mol Cancer Ther (2015). Figure 3. AZD4547 |
| Method | Western blot | |
| Cell Lines | AN3-CA cells | |
| Concentrations | 300 nmol/L | |
| Incubation Time | 2 h | |
| Results | Among 45 transcription factors, four transcription factors were significantly (P < 0.05) perturbed by AZD4547 |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cell line |
| Preparation method | In vitro cell-cycle and apoptotic induction analysis Cell lines were incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells were fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell-cycle profiles were assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media were gently harvested and centrifuged, followed by washing of cell pellets. Cells were then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake according to the manufacturer's instructions. The proportion of cells staining positive for Annexin V were then assessed with a FACSCalibur instrument and quadrant sorting was done by CellQuest analysis software. |
| Concentrations | 0.003~1 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | nude mice bearing established Calu-6 human tumor xenografts |
| Formulation | formulated in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water |
| Dosages | 1.5–50 mg/kg once daily or twice daily |
| Administration | oral gavage |
| Molecular Weight | 463.58 |
| Formula | C26H33N5O3 |
| CAS Number | 1035270-39-3 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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