| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Purine synthesis pathways; thiopurine metabolism. 6-Methylmercaptopurine riboside is a thiopurine nucleoside involved in the inhibition of purine synthesis. It is used to study thiopurine metabolism by enzymes. As a purine nucleoside analog, it interferes with nucleic acid synthesis.
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|---|---|
| ln Vitro |
6-Methylmercaptopurine riboside demonstrates activity in studies on thiopurine metabolism. It exhibits anti-viral effects against various viruses. As a purine nucleoside analog, it would be expected to have anticancer activity. Detailed IC50 values have not been disclosed.
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| ln Vivo |
6-Methylmercaptopurine riboside exhibits anti-viral effects against various viruses. As a thiopurine nucleoside, it would be expected to have activity in animal models of cancer or viral infection. In vivo studies would be needed to evaluate its therapeutic potential.
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| Enzyme Assay |
In vitro assays for thiopurine metabolism involve incubating the compound with enzymes (e.g., thiopurine methyltransferase, xanthine oxidase) and measuring metabolite formation by HPLC or mass spectrometry. For antiviral activity, standard antiviral assays are used.
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| Cell Assay |
Cells (e.g., cancer cell lines or virus-infected cells) are cultured and treated with 6-Methylmercaptopurine riboside at concentrations typically ranging from 0.1–100 μM for 24–72 hours. Purine synthesis inhibition is assessed by measuring nucleotide levels. Cell viability and viral replication are evaluated by standard assays.
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| Animal Protocol |
In vivo animal studies for 6-Methylmercaptopurine riboside have not been extensively reported. The compound is primarily used as a research tool for thiopurine metabolism studies. Future studies in animal models would be needed to evaluate in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 6-Methylmercaptopurine riboside have not been published. The compound has a molecular weight of 298.32 and formula C11H14N4O4S. As a nucleoside analog, it is expected to be taken up by cells via nucleoside transporters. In vivo PK parameters have not been characterized.
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| Toxicity/Toxicokinetics |
Toxicity Data
Rat (intraperitoneal injection): LD50: 65 mg/kg Toxicology data for 6-Methylmercaptopurine riboside have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling thiopurines should be observed. |
| References | |
| Additional Infomation |
6-Methylmercaptopurine nucleoside is a white powder. (NTP, 1992)
6-Methylthioinosine is a thiopurine, a derivative of inosine formed by replacing the aromatic hydroxyl group with a methylthiodiyl group. It is a purine ribonucleotide and also a thiopurine. It is an analog of inosine, with the hydroxyl group at the 6-position replaced by a methylthio group. Methylmercaptopurine nucleoside is a purine derivative with antitumor and anti-angiogenic properties. 6-Methylmercaptopurine nucleoside (6-MMPR) inhibits amide phosphoribosyltransferase (a key first step in the de novo synthesis of purines) and inhibits fibroblast growth factor-2 (FGF2)-induced cell proliferation. (NCI04) 6-(methylthio)-9-β-D-furanose ribosylpurine. An analog of inosine, with the hydroxyl group at the 6-position replaced by a methylthio group. 6-Methylmercaptopurine riboside (CAS: 342-69-8, molecular formula C11H14N4O4S, molecular weight 298.32) is a thiopurine nucleoside analog. It is used in studies on thiopurine metabolism. It exhibits anti-viral effects. It is not in clinical trials. |
| Molecular Formula |
C11H14N4O4S
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|---|---|
| Molecular Weight |
298.32
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| Exact Mass |
298.074
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| CAS # |
342-69-8
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| PubChem CID |
9570
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| Appearance |
White to off-white solid powder
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| Density |
1.85g/cm3
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| Boiling Point |
636.3ºC at 760mmHg
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| Melting Point |
166°C
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| Flash Point |
338.6ºC
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| Index of Refraction |
1.822
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
352
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CSC1=NC=NC2=C1N=CN2[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O
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| InChi Key |
ZDRFDHHANOYUTE-IOSLPCCCSA-N
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| InChi Code |
InChI=1S/C11H14N4O4S/c1-20-10-6-9(12-3-13-10)15(4-14-6)11-8(18)7(17)5(2-16)19-11/h3-5,7-8,11,16-18H,2H2,1H3/t5-,7-,8-,11-/m1/s1
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| Chemical Name |
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-(6-methylsulfanylpurin-9-yl)oxolane-3,4-diol
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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: ~100 mg/mL (~335.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3521 mL | 16.7605 mL | 33.5211 mL | |
| 5 mM | 0.6704 mL | 3.3521 mL | 6.7042 mL | |
| 10 mM | 0.3352 mL | 1.6761 mL | 3.3521 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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