AZ683
Based on 1 Customer Validation
AZ683 is a potent and selective 3-amido-4-anilinoquinoline CSF1R inhibitor. AZ683 has high affinity for CSF1R (Ki=8 nM; IC50=6 nM). AZ683 has good oral bioavailability. [11C]AZ683 can be used as a positron emission tomography (PET) radiotracer for colony stimulating factor 1 receptor (CSF1R).
For research use only. We do not sell to patients.
- Purity: 98.57%
- CAS No.: 953798-95-3
- Formula: C23H25F2N5O2
- Molecular Weight:441.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 6 nM (CSF1R)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
0.23 μM
Compound: 1, AZ683
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Antiproliferative activity against CSF-1-stimulated mouse 3T3 cells expressing CSF1R
Antiproliferative activity against CSF-1-stimulated mouse 3T3 cells expressing CSF1R
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[PMID: 23842474] |
Chemical Information
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CAS No. 953798-95-3
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Appearance Solid
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Molecular Weight 441.47
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Formula C23H25F2N5O2
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Color White to light yellow
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SMILES
O=C(C1=CN=C2C=C(C(N3CCN(CC3)C)=CC2=C1NC4=CC=C(C=C4F)F)OCC)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (113.26 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.33 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Tanzey SS, et al. Synthesis and Initial In Vivo Evaluation of [11C]AZ683-A Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R). Pharmaceuticals (Basel). 2018 Dec 13;11(4):136. [Content Brief]
[2]. Scott DA, et al. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2652 mL | 11.3258 mL | 22.6516 mL | 56.6290 mL |
| 5 mM | 0.4530 mL | 2.2652 mL | 4.5303 mL | 11.3258 mL | |
| 10 mM | 0.2265 mL | 1.1326 mL | 2.2652 mL | 5.6629 mL | |
| 15 mM | 0.1510 mL | 0.7551 mL | 1.5101 mL | 3.7753 mL | |
| 20 mM | 0.1133 mL | 0.5663 mL | 1.1326 mL | 2.8314 mL | |
| 25 mM | 0.0906 mL | 0.4530 mL | 0.9061 mL | 2.2652 mL | |
| 30 mM | 0.0755 mL | 0.3775 mL | 0.7551 mL | 1.8876 mL | |
| 40 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4157 mL | |
| 50 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1326 mL | |
| 60 mM | 0.0378 mL | 0.1888 mL | 0.3775 mL | 0.9438 mL | |
| 80 mM | 0.0283 mL | 0.1416 mL | 0.2831 mL | 0.7079 mL | |
| 100 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL |
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