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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.57%
- CAS 番号: 953798-95-3
- 分子式: C23H25F2N5O2
- 分子量:441.47
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
IC50: 6 nM (CSF1R)[1]
Cellular Effect
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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] |
体外実験
化学情報
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CAS 番号 953798-95-3
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性状 Solid
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分子量 441.47
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
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データシート (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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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 |
AZ683 関連分類
HY-159108 関連分類
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