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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.
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
6-Thio-2'-deoxyguanosine; Beta-TGdR; 6-thio-dG; 6thiodG; 6 thio dG; BetaTGdR; Beta TGdR
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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.
Cancer Discov. 2015 Jan;5(1):82-95.
Purity ≥98%
COA
MSDS