1. Protein Tyrosine Kinase/RTK
  2. FGFR

AZD4547 

Cat. No.: HY-13330 Purity: 99.80%
Handling Instructions

AZD4547 is a potent inhibitor of the FGFR family with IC50 of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

For research use only. We do not sell to patients.

AZD4547 Chemical Structure

AZD4547 Chemical Structure

CAS No. : 1035270-39-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 168 In-stock
Estimated Time of Arrival: December 31
100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
200 mg USD 324 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

View All FGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AZD4547 is a potent inhibitor of the FGFR family with IC50 of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

IC50 & Target[1]

FGFR1

0.2 nM (IC50)

FGFR2

2.5 nM (IC50)

FGFR3

1.8 nM (IC50)

FGFR4

165 nM (IC50)

In Vitro

AZD4547 also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC50 of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, AZD4547 potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC50 values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC50=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC50 values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, AZD4547 potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level[1].

In Vivo

Female SCID mice bearing KMS11 tumors are randomized and treated chronically with AZD4547 at a range of well-tolerated doses. Oral AZD4547 treatment results in dose-dependent tumor growth inhibition. Twice daily administration of AZD4547 at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily AZD4547 results in 65% tumor growth inhibition (P=0.002)[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 300 mg/mL (647.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1572 mL 10.7859 mL 21.5717 mL
5 mM 0.4314 mL 2.1572 mL 4.3143 mL
10 mM 0.2157 mL 1.0786 mL 2.1572 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Cells are treated with AZD4547 or control for 3 hours at 37°C and then stimulated with 10 ng/mL aFGF/bFGF and 10 μg/mL heparin for 20 minutes. Western blotting is conducted with standard SDS-PAGE procedures and antibody incubation carried out overnight at 4°C. Antibodies are obtained from the following sources: FGFR1, FGFR2 and FRS2, FGFR3 proteins, α-tubulin-B512 and Bcl2 (C2), and BIM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cell lines are incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells are fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell-cycle profiles are assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media are gently harvested and centrifuged, followed by washing of cell pellets. Cells are then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake. The proportion of cells staining positive for Annexin V are then assessed with a FACSCalibur instrument and quadrant sorting is done by CellQuest analysis software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Swiss derived nude (nu/nu) and severe combined immunodeficient mice (SCID) are used. Tumor xenografts are established by s.c. injection into the left flank with 0.1 mL tumor cells (1×106 for LoVo, 1×107 for HCT-15, and 1×107 for Calu-6) or 0.2 mL (2×107 for KMS11 and KG1a) mixed 1:1 with Matrigel, with the exception of LoVo and HCT-15, which do not include Matrigel. Mice are randomized into control and treatment groups (AZD4547, 1.5-50 mg/kg, once daily or twice daily by oral gavage) when tumors reach the determined size of more than 0.2 cm3. Tumor volume (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Tumor volume is calculated.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

463.57

Formula

C₂₆H₃₃N₅O₃

CAS No.

1035270-39-3

SMILES

C[[email protected]](C1)N[[email protected]@H](C)CN1C2=CC=C(C(NC3=NNC(CCC4=CC(OC)=CC(OC)=C4)=C3)=O)C=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.80%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZD4547
Cat. No.:
HY-13330
Quantity:

AZD4547

Cat. No.: HY-13330