| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Purity: ≥98%
CGS 15943 is a novel, potent and selective adenosine receptor antagonist with Ki values of 3.5, 4.2, 16 and 51 nM for human A1, A2A, A2B and A3 receptors respectively.
| ln Vitro |
CGS 15943 slightly inhibits p110δ with an IC50 of 8.47 μM and suppresses the intermittent activity of class IB PI3K isoform p110γ with an IC50 of 1.1 μM [3]. HLF and SK-Hep are inhibited by CGS 15943 (0–20 μM; 72 hours). CGS 15943 (0 -20 μM; 24 hours) inhibits the development of HepG2 and PLC-PRF-5 cells [3] as well as the phosphorylation of Akt residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells [3].
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| Cell Assay |
Cell viability assay [3]
Cell Types: HLF, SK-Hep-1, HepG2 and PLC-PRF-5 Cell Tested Concentrations: 0 μM; ]. 1μM; 5μM; 10μM; 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the growth of four different HCC cell lines. Western Blot Analysis[3] Cell Types: HLF and Sk-Hep-1 cells Tested Concentrations: 0 μM; 1μM; 5μM; 10μM; 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of PI3K/ in HLF and Sk-Hep-1 cells Akt pathway |
| References |
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| Additional Infomation |
CGS 15943 is a member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors. It has a role as an adenosine A1 receptor antagonist, an adenosine A2A receptor antagonist, a central nervous system stimulant and an antineoplastic agent. It is a triazoloquinazoline, an organochlorine compound, a member of furans, a biaryl, an aromatic amine and a primary amino compound.
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| Molecular Formula |
C13H8CLN5O
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|---|---|
| Molecular Weight |
285.68852
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| Exact Mass |
285.042
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| CAS # |
104615-18-1
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| PubChem CID |
2690
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| Appearance |
White to off-white solid powder
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| Density |
1.72 g/cm3
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| Boiling Point |
566.6ºC at 760 mmHg
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| Melting Point |
278-279 °C
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| Flash Point |
296.5ºC
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| Vapour Pressure |
7.4E-13mmHg at 25°C
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| Index of Refraction |
1.84
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| LogP |
3.354
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
373
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MSJODEOZODDVGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)
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| Chemical Name |
9-chloro-2-furan-2-yl-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
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| Synonyms |
CGS 15943 CGS15943 CGS-15943.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.22 mg/mL (~42.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.22 mg/mL (4.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.22 mg/mL (4.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.22 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5003 mL | 17.5015 mL | 35.0030 mL | |
| 5 mM | 0.7001 mL | 3.5003 mL | 7.0006 mL | |
| 10 mM | 0.3500 mL | 1.7501 mL | 3.5003 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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