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AZD4547

Cat. No. M1721
AZD4547 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 57  USD57 In stock
10mg USD 74  USD74 In stock
50mg USD 168  USD168 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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
Protocol
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 (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).
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 463.58
Formula C26H33N5O3
CAS Number 1035270-39-3
Purity 99.83%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

[1] 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.

[2] Gavine et al. Cancer Res. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family.

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Keywords: AZD4547 supplier, FGFR, inhibitors

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