AZD4547 (Synonyms: AZD 4547;AZD-4547) |
Catalog No.GC14005
One-Click Copy Product Info
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FGFR inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1035270-39-3
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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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]: | |
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Cell lines |
KG1a, Sum52-PE, KMS11 and MCF7 cells |
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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. |
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Reacting condition |
1 μM; 72 hrs |
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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]: | |
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Animal models |
SCID mice bearing KMS11 tumors |
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Dosage form |
1.5 ~ 12.5 mg/kg, p.o.; q.d. or b.i.d. |
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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. |
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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. |
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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. | |
| Cas No. | 1035270-39-3 | 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1572 mL | 10.7859 mL | 21.5717 mL |
| 5 mM | 431.4 μL | 2.1572 mL | 4.3143 mL |
| 10 mM | 215.7 μL | 1.0786 mL | 2.1572 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)