AZD4547 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
|Source||Mol Cancer Ther (2015). Figure 3. AZD4547|
|Cell Lines||AN3-CA cells|
|Incubation Time||2 h|
|Results||Among 45 transcription factors, four transcription factors were significantly (P < 0.05) perturbed by AZD4547|
|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 (Sigma) labeling solution. Cell-cycle profiles were assessed with a FACSCalibur instrument and CellQuest analysis software (Becton Dickinson). 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 (Abcam). 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 (Becton Dickinson).
|Incubation time||72 h|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 80 mg/mL|
 Chell et al. Oncogene. Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance.
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