| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Alpha-Guanosine acts as a purine nucleoside analog. It is not a specific enzyme inhibitor; rather, it can be incorporated into nucleic acids or interfere with nucleotide metabolism. Its anticancer mechanism relies on inhibiting DNA synthesis and inducing apoptosis in cancer cells.
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| ln Vitro |
In vitro, Alpha-Guanosine has demonstrated broad-spectrum anticancer activity, particularly against indolent lymphoid malignancies. As a purine nucleoside analog, it targets rapidly dividing cells by being incorporated into DNA during replication. This process leads to DNA strand breaks and triggers programmed cell death (apoptosis). It has a similar mechanism to other drugs in this class.
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| ln Vivo |
The in vivo anticancer activity is inferred from its mechanism. Purine nucleoside analogs like fludarabine are established therapies for leukemia. While specific in vivo efficacy data for alpha-guanosine is not provided, research into alpha-nucleosides explores their potential for use in gene regulation and as therapeutics for cancer and neurodegenerative disorders. Further studies are needed.
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| Enzyme Assay |
A standard non-cellular assay for a nucleoside analog is its incorporation into DNA by a purified DNA polymerase. In a cell-free reaction, a DNA template, a primer, dNTPs, and the DNA polymerase (e.g., Taq polymerase) are mixed with varying concentrations of alpha-guanosine triphosphate (the triphosphate form of the analog). The reaction is run, and the resulting DNA products are analyzed by gel electrophoresis. The compound is expected to cause chain termination or mutations.
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| Cell Assay |
To assess its anticancer activity, an in vitro cytotoxicity assay using cancer cell lines is performed. A panel of human lymphoma or leukemia cell lines (e.g., Jurkat, Raji) is treated with serial dilutions of Alpha-Guanosine for 72 hours. Cell viability is measured using a colorimetric assay like MTT or CellTiter-Glo. The IC₅0 (the concentration that kills 50% of the cells) is calculated. A flow cytometry assay using Annexin V and PI can be used to confirm that the cell death is due to apoptosis.
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| Animal Protocol |
Specific in vivo protocols are not provided. A typical study would involve a mouse xenograft model of lymphoma. Immunodeficient mice are injected subcutaneously with a human lymphoma cell line. Once tumors become palpable, mice are randomized into treatment and control groups. Alpha-Guanosine is administered by intraperitoneal (IP) injection daily. Tumor growth is monitored with calipers. Mice are euthanized when tumors reach a pre-determined size, and the tumors are excised for analysis. Survival time is also a key endpoint.
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| ADME/Pharmacokinetics |
PK properties for the alpha-anomer are expected to be different from natural guanosine. It may be more resistant to degradation by nucleotidases and less efficiently recognized by cellular transporters. Its bioavailability and half-life would determine its potential as a drug. These properties are typically characterized in pre-clinical PK studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available. As a nucleoside analog, it could cause bone marrow suppression, gastrointestinal toxicity, and immunosuppression, which are class effects. These toxicities are often dose-limiting in the clinic. Its anomeric configuration might alter its toxicity profile.
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| References | |
| Additional Infomation |
The anomeric configuration creates a molecule that mimics but is not a perfect substrate for natural enzymes. This is a classic strategy in medicinal chemistry to create "anti-metabolites" that hijack cellular machinery. It is used primarily as a research tool to study nucleic acid metabolism and the structural requirements of polymerases. It is not a standard clinical drug but a scaffold for drug discovery.
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| Molecular Formula |
C10H13N5O5
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|---|---|
| Molecular Weight |
283.240721464157
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| Exact Mass |
283.091
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| CAS # |
15398-66-0
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| PubChem CID |
136912867
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| Appearance |
White to off-white solid powder
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| LogP |
-1.9
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
446
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=NC2=C(N1[C@@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N=C(NC2=O)N
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| InChi Key |
NYHBQMYGNKIUIF-BDXYJKHTSA-N
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| InChi Code |
InChI=1S/C10H13N5O5/c11-10-13-7-4(8(19)14-10)12-2-15(7)9-6(18)5(17)3(1-16)20-9/h2-3,5-6,9,16-18H,1H2,(H3,11,13,14,19)/t3-,5-,6-,9+/m1/s1
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| Chemical Name |
2-amino-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-purin-6-one
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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 : 12.5 mg/mL (44.13 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5306 mL | 17.6529 mL | 35.3057 mL | |
| 5 mM | 0.7061 mL | 3.5306 mL | 7.0611 mL | |
| 10 mM | 0.3531 mL | 1.7653 mL | 3.5306 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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