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    6-Thio-dG (β-TGdR)
    6-Thio-dG (β-TGdR)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1427
    CAS #: 789-61-7Purity ≥98%

    Description: 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 is used as an anti-cancer agent. Cancer cells were very sensitive to 6-thio-dG with observed IC50 values ranging from 0.7-2.9 μM, depending on cell types. 6-Thio-dG induces telomere dysfunction and results in progressive telomere shortening in telomerase-positive human cancer cells and hTERT-expressing human fibroblasts. In tested cancer cells, 6-thio-dG inhibits cell viability with IC50 values between 0.7 and 2.9 μM.

    References: Cancer Discov. 2015 Jan;5(1):82-95.

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    Molecular Weight (MW)283.31
    FormulaC10H13N5O3S 
    CAS No.789-61-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 56 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)

    Chemical Name: 2-Amino-9-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purine-6-thione

    InChi Key: SCVJRXQHFJXZFZ-KVQBGUIXSA-N

    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

    SMILES Code: S=C1N=C(N)NC2=C1N=CN2[[email protected]@H]3O[[email protected]](CO)[[email protected]@H](O)C3

    Synonyms

    6-Thio-2'-deoxyguanosine; Beta-TGdR; 6-thio-dG; 6thiodG; 6 thio dG; BetaTGdR; Beta TGdR


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    In Vitro

    In vitro activity: 6-Thio-dG induces telomere dysfunction and results in progressive telomere shortening in telomerase-positive human cancer cells and hTERT-expressing human fibroblasts. In tested cancer cells, 6-thio-dG inhibits cell viability with IC50 values between 0.7 and 2.9 μM.


    Cell Assay: Cells (HCT11, A549, H2882, HCC2429, HCC827, HCC15, H2087, HCC4017, HCC515, H2009, BJ and HCEC1 cells) are plated in growth media in 96-well plates. Cells are incubated for 1 week and treated with varying concentrations of 6-thio-dG and 6-thioguanine or DMSO every 3 days. The 96-well plates are analyzed according the manufacturer’s directions for the CellTiterGlo luminescent cell viability assay to obtain IC50 values. The IC50 is defined as the concentration of drug at which 50% of the cells are inhibited by the drug. Sigmoidal dose–response curves are used to calculate IC50 values. All samples are analyzed in triplicate, and SDs are from two independent experiments.

    In VivoIn mice bearing A549 lung cancer xenografts, 6-Thio-dG (2 mg/kg, i.p.) decreases the tumorigenicity of A549 Cells by inducing telomere dysfunction.
    Animal modelMice bearing A549 lung cancer xenografts
    Formulation & DosageDissolved in 5% DMSO solution; 2 mg/kg; i.p. injection
    References

    Cancer Discov. 2015 Jan;5(1):82-95.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    6-Thio-dG

    TRF (Terminal Restriction Fragment) and TRAP (Telomeric Repeat Amplification Protocol) analysis. Cancer Discov. 2015 Jan;5(1):82-95.
     

    6-Thio-dG

    Intraperitoneally or intratumorally injection of 6-thio-dG or 6-thioguanine (5A) 2mg/kg 6-thio-dG or 6-thioguanine injected to the A549-derived tumor for 17 days every two days, intraperitoneally. Cancer Discov. 2015 Jan;5(1):82-95.


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