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Purity: ≥98%
6-thio-dG (β-TGdR; 6-Thio-2'-Deoxyguanosine; BetaTGdR) is a nucleoside analog and a potent telomerase-mediated telomere disrupting compound with potential antitumor activity. It has anti-cancer properties. The observed IC50 values of cancer cells ranged from 0.7-2.9 μM, indicating high sensitivity to 6-thio-dG. 6-In telomerase-positive human cancer cells and hTERT-expressing human fibroblasts, Thio-dG causes telomere dysfunction and progressive telomere shortening. 6-thio-dG has been found to inhibit cell viability in tested cancer cells, with IC50 values ranging from 0.7 to 2.9 μM.
| Targets |
DNA/RNA Synthesis
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| Cell Assay |
In 96-well plates, cells are plated in growth media. After a week of incubation, the cells are treated every three days with DMSO or different concentrations of 6-thio-dG and 6-thioguanine. To determine the IC50 values for the CellTiterGlo luminescent cell viability assay, the 96-well plates are analyzed in accordance with the manufacturer's instructions. The drug concentration at which 50% of cells are inhibited by the drug is known as the IC50. To determine IC50 values, sigmoidal dose-response curves are utilized. The SDs are derived from two separate experiments, and each sample is examined in triplicate.
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
THE PHARMACOKINETICS OF RADIOLABELED 6-THIOGUANINE (TG) WERE COMPARED WITH THAT OF BETA-2'-DEOXYTHIOGUANOSINE (BETA-TGDR) AFTER IV ADMIN. URINARY EXCRETION OF THE RADIOLABEL WAS 75% OF THE DOSE 24 HR AFTER ADMIN. BOTH THIOPURINES WERE RAPIDLY & EXTENSIVELY DEGRADED & EXCRETED AS 6-THIOXANTHINE, INORGANIC SULFATE, S-METHYL-6-THIOXANTHINE, & 6-THIOURIC ACID IN ADDITION TO OTHER PRODUCTS. SMALL AMOUNTS OF UNCHANGED DRUG WERE ALSO EXCRETED. STUDIES SUGGEST THAT BETA-TGDR IS A LATENT FORM OF TG. SINCE RESISTANCE TO ANTILEUKEMIC AGENT 6-THIOGUANINE INEVITABLY DEVELOPS IN ANIMAL TUMORS, THIS NEW AGENT BETA-TGDR IS OF POTENTIAL CLINICAL USE. |
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| References | ||
| Additional Infomation |
Beta-Thioguanine Deoxyriboside is a thiopurine nucleoside derivative with antineoplastic activity. After conversion to the triphosphate, beta-thioguanine deoxyriboside is incorporated into DNA, resulting in inhibition of DNA replication. This agent is cytotoxic against leukemia cell lines and has demonstrated some activity against leukemia cells in vivo. Beta-thioguanine deoxyriboside demonstrates antineoplastic activity against 6-thioguanine-resistant tumor cells. (NCI04)
See also: 6-Thioguanosine (annotation moved to). Therapeutic Uses STUDIES SUGGEST THAT BETA-TGDR IS A LATENT FORM OF TG. SINCE RESISTANCE TO ANTILEUKEMIC AGENT 6-THIOGUANINE INEVITABLY DEVELOPS IN ANIMAL TUMORS, THIS NEW AGENT BETA-TGDR IS OF POTENTIAL CLINICAL USE. |
| Molecular Formula |
C10H13N5O3S
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| Molecular Weight |
283.31
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| Exact Mass |
283.073
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| Elemental Analysis |
C, 42.40; H, 4.63; N, 24.72; O, 16.94; S, 11.32
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| CAS # |
789-61-7
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| Related CAS # |
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| PubChem CID |
3000603
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| Appearance |
White to yellow solid powder
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| Density |
2.0±0.1 g/cm3
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| Boiling Point |
709.1±70.0 °C at 760 mmHg
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| Flash Point |
382.6±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.930
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| LogP |
-0.91
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
420
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S=C1N=C(N)NC2N([C@H]3C[C@H](O)[C@@H](CO)O3)C=NC1=2
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| InChi Key |
SCVJRXQHFJXZFZ-KVQBGUIXSA-N
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| InChi Code |
InChI=1S/C10H13N5O3S/c11-10-13-8-7(9(19)14-10)12-3-15(8)6-1-4(17)5(2-16)18-6/h3-6,16-17H,1-2H2,(H3,11,13,14,19)/t4-,5+,6+/m0/s1
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| Chemical Name |
2-amino-9-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purine-6-thione
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| Synonyms |
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (2.93 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 8.3 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: ≥ 0.83 mg/mL (2.93 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 | 3.5297 mL | 17.6485 mL | 35.2970 mL | |
| 5 mM | 0.7059 mL | 3.5297 mL | 7.0594 mL | |
| 10 mM | 0.3530 mL | 1.7649 mL | 3.5297 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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