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AZD4547FGFR inhibitor

AZD4547

Catalog No. A8350
Size Price Stock Qty
10mM (in 1mL DMSO) $90.00 In stock
Evaluation Sample $28.00 In stock
5mg $80.00 In stock
10mg $120.00 In stock
50mg $250.00 In stock
100mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AZD4547

Related Biological Data

AZD4547

Related Biological Data

AZD4547

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      

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.

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Chemical Properties

Cas No. 1035270-39-3 SDF Download SDF
Synonyms AZD 4547;AZD-4547
Chemical Name N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide
Canonical SMILES CC1CN(CC(N1)C)C2=CC=C(C=C2)C(=O)NC3=NNC(=C3)CCC4=CC(=CC(=C4)OC)OC
Formula C26H33N5O3 M.Wt 463.57
Solubility >23.2mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

AZD4547 is a potent, specific, orally bioavailable fibroblast growth factors receptor (FGFR) tyrosine kinase inhibitor. It inhibits FGFR1, FGFR2, and FGFR3 with IC50 values of 12, 2 and 40 nM, respectively. AZD4547 has also been reported to block FGFR1, FGFR2, and FGFR3 autophosphorylation with IC50 values of 0.2, 2.5, and 1.8 nM, respectively [1].

AZD4547 has been demonstrated to inhibit cell proliferation and inhibit FGFRs and their downstream markers including PLCg and FRS2 phosphorylation in breast cell line Sum52-PE (expressing wild-type FGFR2), multiple myeloma line KMS11 (expressing Y373C mutated FGFR3 protein) and acute myeloid leukemia cell line KG1a (expressing wild-type FGFR1) [1].

Anti-carcinoma effect of AZD4547 has been observed in lung cancer xeonograft mice orally treated with AZD4547. This effect is believed to be via the specifically inhibition of the activity of FGFR but not kinase insert domain receptor (KDR)[1].

References:
[1] Gavine PR1,?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.