CGS 15943
Based on 1 Customer Validation
CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
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- Pureza: 99.55%
- No. CAS: 104615-18-1
- Fòrmula: C13H8ClN5O
- Peso molecular:285.69
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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p110γ 1.1 μM (IC50) |
p110δ 8.47 μM (IC50) |
adenosine A1 receptor 3.5 nM (Ki) |
adenosine A2A receptor 4.2 nM (Ki) |
adenosine A2B receptor 16 nM (Ki) |
adenosine A3 receptor 50 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
1.2 μM
Compound: 1a
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Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
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[PMID: 9667972] |
| CHO | IC50 |
406 nM
Compound: CGS-15943
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Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor
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[PMID: 11123985] |
CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ with an IC50 of 1.1 μM and shows slight inhibition on p110δ with an IC50 of 8.47 μM[3]. CGS 15943 (0-20 μM; 72 hours) inhibits growth of HLF and SK-Hep-1 cells, as well as HepG2 and PLC-PRF-5 cells[3]. CGS 15943 (0-20 μM; 24 hours) reduces the phosphorylation of Akt at its residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HLF, SK-Hep-1, HepG2 and PLC-PRF-5 cells
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Concentration:0 μM; 1 μM; 5 μM; 10 μM; 20 μM
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Incubation Time:24 hours
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Result:Inhibited growth of four distinct HCC cell lines.
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Cell Line:HLF and Sk-Hep-1 cells
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Concentration:0 μM; 1 μM; 5 μM; 10 μM; 20 μM
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Incubation Time:24 hours
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Result:Inhibited the PI3K/Akt pathway in HLF and Sk-Hep-1 cells
Chemical Information
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No. CAS 104615-18-1
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Appearance Solid
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Peso molecular 285.69
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Fòrmula C13H8ClN5O
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Color White to off-white
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SMILES
NC1=NC2=C(C=C(Cl)C=C2)C3=NC(C4=CC=CO4)=NN13
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 12.22 mg/mL (42.77 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: 1.22 mg/mL (4.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.22 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.2 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.22 mg/mL (4.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.22 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gao Y, et al. CGS 15943, an adenosine A2 receptor antagonist, reduces cerebral ischemic injury in the Mongolian gerbil. Life Sci. 1994;55(3):PL61-5. [Content Brief]
[2]. Klotz KN, et al. Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91. [Content Brief]
[3]. Edling CE, et al. Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol Ther. 2014 May;15(5):524-32. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5003 mL | 17.5015 mL | 35.0030 mL | 87.5074 mL |
| 5 mM | 0.7001 mL | 3.5003 mL | 7.0006 mL | 17.5015 mL | |
| 10 mM | 0.3500 mL | 1.7501 mL | 3.5003 mL | 8.7507 mL | |
| 15 mM | 0.2334 mL | 1.1668 mL | 2.3335 mL | 5.8338 mL | |
| 20 mM | 0.1750 mL | 0.8751 mL | 1.7501 mL | 4.3754 mL | |
| 25 mM | 0.1400 mL | 0.7001 mL | 1.4001 mL | 3.5003 mL | |
| 30 mM | 0.1167 mL | 0.5834 mL | 1.1668 mL | 2.9169 mL | |
| 40 mM | 0.0875 mL | 0.4375 mL | 0.8751 mL | 2.1877 mL |
CGS 15943 Related Classifications
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