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AZD4547

Catalog No.
A8350
FGFR inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$88.00
In stock
Evaluation Sample
$30.00
In stock
5mg
$73.00
In stock
10mg
$101.00
In stock
50mg
$189.00
In stock
100mg
$276.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

AZD4547 (CAS: 1035270-39-3) is an orally bioavailable inhibitor targeting fibroblast growth factor receptors (FGFRs). It selectively inhibits FGFR1, FGFR2, and FGFR3 tyrosine kinase activities, exhibiting IC50 values of 12 nM, 2 nM, and 40 nM, respectively, and potently reduces their autophosphorylation. AZD4547 treatment in breast cancer (Sum52-PE), multiple myeloma (KMS11), and acute myeloid leukemia (KG1a) cells decreases proliferation and FGFR downstream signal phosphorylation. Preclinical studies in lung cancer xenograft models illustrate its antitumor efficacy associated with selective FGFR inhibition, highlighting its research utility in studying FGFR-related oncology.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt463.57
Cas No.1035270-39-3
FormulaC26H33N5O3
SynonymsAZD 4547;AZD-4547
Solubility≥23.2 mg/mL in DMSO; insoluble in H2O; ≥6.33 mg/mL in EtOH
Chemical NameN-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide
SDFDownload SDF
Canonical SMILESCC1CN(CC(N1)C)C2=CC=C(C=C2)C(=O)NC3=NNC(=C3)CCC4=CC(=CC(=C4)OC)OC
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Kinase experiment [1]:

AZD4547 kinase activity

The ability of AZD4547 to inhibit the human recombinant kinase activities of FGFR1-3 was tested using ATP concentrations at, or just below, the respective Km.

Cell experiment [1]:

Cell lines

KG1a, Sum52-PE, KMS11 and MCF7 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM; 72 hrs

Applications

AZD4547 affected AKT phosphorylation in Sum52-PE and MCF7 cells, but not in KG1a and KMS11 cells. AZD4547 treatment significantly induced apoptosis in Sum52-PE and KMS11 cells, and dramatically increased G1 arrest but not apoptosis in KG1a cells. In MCF7 cells, AZD4547 showed no effect on cell cycle distribution or apoptosis.

Animal experiment [1]:

Animal models

SCID mice bearing KMS11 tumors

Dosage form

1.5 ~ 12.5 mg/kg, p.o.; q.d. or b.i.d.

Applications

In mice bearing KMS11 tumors, AZD4547 (3 mg/kg, b.i.d.) significantly inhibited tumor growth (53%). AZD4547 treatment at 12.5 mg/kg once daily or 6.25 mg/kg twice daily resulted in complete tumor stasis due to dose-dependent modulation of phospho-FGFR3, and reduced KMS11 cell proliferation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Gavine PR, Mooney L, Kilgour E, Thomas AP, Al-Kadhimi K, Beck S, Rooney C, Coleman T, Baker D, Mellor MJ, Brooks AN, Klinowska T. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res.2012 Apr 15;72(8):2045-56.

Biological Activity

Description AZD4547 is a novel selective inhibitor of FGFR for FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38.
Targets FGFR1 FGFR2 FGFR3      
IC50 0.2 nM 2.5 nM 1.8 nM      

Quality Control

Chemical structure

AZD4547

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AZD4547

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