6-Thio-dG
(Synonyms: 6-巯基-2'-脱氧鸟苷,β-TGdR; 6-Thio-2'-Deoxyguanosine) 目录号 : GC12193
A purine nucleoside analog
Cas No.:789-61-7
Sample solution is provided at 25 µL, 10mM.
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6-thio-dG is a nucleoside analogue [1], is a telomerase-mediated telomere disrupting compound [2]. It is an anti-cancer inhibitor [1]. Cancer cells were very sensitive to 6-thio-dG with observed IC50 values ranging from 0.7-2.9 μM, depending on cell types [3].
Telomeres are found at the end of eukaryotic linear chromosomes. They are essential for genomic stability and chromosome maintenance [3].
In HCT116 human colon cancer cell line, treatment with 6-thio-dG made progressive telomere shortening independent of telomerase activity inhibition and induced telomere dysfunction. GRN163L is a telomerase inhibitor. In HCT116 cells, treatment with GRN163L and 6-thio-dG together increased telomere shortening. Within 1 week, 6-thio-dG killed most of HCT116 cells and altered cellular morphology. Normal BJ fibroblast cells are telomerase silent. After 1 week, treatment with 6-thio-dG showed no effect on cell morphology. After long-term treatment with 6-thio-dG, no effect on telomere shortening was found [1].
In murine mode with xenograft derived from A549 lung cancer cell line, as compared to controls, intraperitoneal injection with 2 mg/kg of 6-thio-dG every other day completely prevented progressive tumor growth. Ki67 is a biomarker correlating with proliferation levels. Compared to controls, 6-thio-dG decreased Ki67 staining. Treatment with 6-thio-dG through local injection resulted in even more dramatic decrease in the tumor growth rate compared to untreated controls [3].
References:
[1]. Mender I, Gryaznov S, Dikmen ZG, et al. Abstract LB-125: A novel telomerase inhibitor. Cancer Research, 2013, 73(8 Supplement): LB-125-LB-125.
[2]. Mender I, Gryaznov S, Shay JW. A novel telomerase substrate precursor rapidly induces telomere dysfunction in telomerase positive cancer cells but not telomerase silent normal cells. Oncoscience, 2015, 2(8): 693.
[3]. Mender I, Gryaznov S, Dikmen ZG, et al. Induction of telomere dysfunction mediated by the telomerase substrate precursor 6-thio-2-deoxyguanosine. Cancer discovery, 2015, 5(1): 82-95.
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Cell experiment: |
HCT116, A549, and 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-2'-Deoxyguanosine and 6-thioguanine or DMSO every three days. The 96 well plates are analyzed for the CellTiterGlo luminescent cell viability assay[1]. |
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Animal experiment: |
Athymic NCR nu/nu female mice (6 weeks old) are used. A549 cells are inoculated subcutaneously into the left and right dorsal flanks of the nude mice in 100 µL phosphate buffered saline (PBS). When tumors reach 40 mm3 average volume, mice are randomly divided into control, 6-thio-dG and 6-thioguanine treatment groups (3 animals in each group). Animals are injected intraperitoneally every two days for 17 days at a dose of 2mg/kg in 100 µL DMSO/PBS mixture per mouse. In addition, different animals are injected intratumorally every day for 16 days at a dose of Athymic NCR nu/nu female mice2.5mg/kg in 50 µL DMSO/PBS mixture per mouse. Tumor size is measured by calipers and recorded either every day or every two days[1]. |
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References: [1]. Mender I, et al. Induction of telomere dysfunction mediated by the telomerase substrate precursor 6-thio-2'-deoxyguanosine. Cancer Discov. 2015 Jan;5(1):82-95. |
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| Cas No. | 789-61-7 | SDF | |
| 别名 | 6-巯基-2'-脱氧鸟苷,β-TGdR; 6-Thio-2'-Deoxyguanosine | ||
| 化学名 | (2R,3S,5R)-2-(hydroxymethyl)-5-(2-imino-6-mercapto-2H-purin-9(3H)-yl)tetrahydrofuran-3-ol | ||
| Canonical SMILES | N=C1NC2=C(N=CN2[C@@]3([H])C[C@@](O)([H])[C@@](O3)([H])CO)C(S)=N1 | ||
| 分子式 | C10H13N5O3S | 分子量 | 283.31 |
| 溶解度 | ≥ 62.5mg/mL in DMSO | 储存条件 | Store at -20°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5297 mL | 17.6485 mL | 35.297 mL |
| 5 mM | 0.7059 mL | 3.5297 mL | 7.0594 mL |
| 10 mM | 0.353 mL | 1.7649 mL | 3.5297 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet