2-Deoxy-D-glucose
(Synonyms: 2-脱氧-D-葡萄糖; 2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose) 目录号 : GC17430
2-Deoxy-D-glucose (2DG)，是一种葡萄糖类似物，作为竞争性糖酵解抑制剂。
Cas No.:154-17-6
Sample solution is provided at 25 µL, 10mM.
2-Deoxy-D-glucose (2DG), is a glucose analogue, act as competitive glycolytic inhibitor [1].
2-Deoxy-d-glucose (2DG) has been demonstrated to be a powerful agent for blocking and probing increased sugar metabolism in cancer cells [2]. Because of its similarity to glucose, 2-Deoxy-D-glucose inhibits glycolysis, but as chemically it is also 2-deoxymannose it is able to compete with mannose in the growing lipid-linked oligosaccharide chain during the initial steps of N-linked glycosylation. This mannose-like property of 2-Deoxy-D-glucose results in misfolded proteins leading to endoplasmic reticulum (ER) stress [3].
2-Deoxy-D-glucose delivered in the diet produces cardiac toxicity in rats at doses ranging from 0.02 to 0.3 g/kg (0.04-0.6% 2-Deoxy-D-glucose by weight in the diet) and hastens mortality at doses above 0.2 g/kg (0.4% in the diet) [4]. 2-Deoxy-D-glucose evoked increases in plasma adrenaline and glucose at 20 and 60 min [5].
References:
[1]. Mühlenberg T, Grunewald S, Treckmann J, et al. Inhibition of KIT-glycosylation by 2-deoxyglucose abrogates KIT-signaling and combination with ABT-263 synergistically induces apoptosis in gastrointestinal stromal tumor[J]. PloS one, 2015, 10(3): e0120531.
[2]. El Mjiyad N, Caro-Maldonado A, Ramirez-Peinado S, Munoz-Pinedo C. Sugar-free approaches to cancer cell killing. Oncogene. 2011 Jan;30(3):253-64.
[3]. Kurtoglu, Metin, Johnathan C. Maher, and Theodore J. Lampidis. "Differential toxic mechanisms of 2-deoxy-D-glucose versus 2-fluorodeoxy-D-glucose in hypoxic and normoxic tumor cells." Antioxidants & redox signaling 9.9 (2007): 1383-1390.
[4]. Minor R K, Smith Jr D L, Sossong A M, et al. Chronic ingestion of 2-deoxy-D-glucose induces cardiac vacuolization and increases mortality in rats[J]. Toxicology and applied pharmacology, 2010, 243(3): 332-339.
[5]. Bobrovskaya L, Damanhuri H A, Ong L K, et al. Signal transduction pathways and tyrosine hydroxylase regulation in the adrenal medulla following glucoprivation: an in vivo analysis[J]. Neurochemistry international, 2010, 57(2): 162-167.
2-Deoxy-D-glucose (2DG)，是一种葡萄糖类似物，作为竞争性糖酵解抑制剂[1]。
2-脱氧-d-葡萄糖 (2DG) 已被证明是一种强大的药物，可阻断和探测癌细胞中增加的糖代谢[2]。由于其与葡萄糖的相似性，2-脱氧-D-葡萄糖抑制糖酵解，但在化学上它也是 2-脱氧甘露糖，它能够在 N-连接糖基化的初始步骤中与生长的脂质连接的寡糖链中的甘露糖竞争. 2-脱氧-D-葡萄糖的这种类似甘露糖的特性导致错误折叠的蛋白质导致内质网 (ER) 应激 [3]。
饮食中提供的 2-脱氧-D-葡萄糖在 0.02 至 0.3 g/kg 的剂量范围内（饮食中 0.04-0.6% 2-脱氧-D-葡萄糖按重量计）对大鼠产生心脏毒性并加速死亡率剂量超过 0.2 g/kg（饮食中的 0.4%）[4]。 2-脱氧-D-葡萄糖在 20 分钟和 60 分钟时引起血浆肾上腺素和葡萄糖的增加[5]。
| Cell experiment [1]: | |
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Cell lines |
Cell lines SkBr3, MCF-7, BT474, and MDA/MB468, |
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Preparation Method |
Cells were plated at 4000 cells well-1 in a 96-well plate, allowed 24 h to attach and subsequently exposed for 4 days to 2-Deoxy-D-glucose. |
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Reaction Conditions |
4-12 mM for 0-4 days |
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Applications |
Growth of MDA/MB468 cells was completely inhibited by treatment with 8 mM 2-Deoxy-D-glucose. Treatment with 4 mM 2-Deoxy-D-glucose resulted in approximately 30% inhibition of cell growth. Of the breast cancer cell lines tested, SkBr3 was the most sensitive to the growth inhibitory effects of 2-Deoxy-D-glucose. Cell growth was completely inhibited at 4 mM 2-Deoxy-D-glucose. |
| Animal experiment [2]: | |
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Animal models |
male Sprague-Dawley (SD) rats |
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Preparation Method |
Animals were handled routinely in order to reduce stress associated with injection. 2-deoxy-d-glucose (400 mg/kg), or saline, was administered intraperitoneally. |
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Dosage form |
Intraperitoneal injection , 400 mg/kg |
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Applications |
Ad concentrations increased from 2.73 ng/ml to 7.2 ng/ml while NAd concentrations increased from 1.8 ng/ml to 3.14 ng/ml after injected 2-deoxy-d-glucose. |
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References: [1]: Aft R L, Zhang F W, Gius D. Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: mechanism of cell death[J]. British journal of cancer, 2002, 87(7): 805-812. |
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| Cas No. | 154-17-6 | SDF | |
| 别名 | 2-脱氧-D-葡萄糖; 2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose | ||
| 化学名 | (4R,5S,6R)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,4,5-triol | ||
| Canonical SMILES | [H][C@]([C@](C1([H])[H])([H])O[H])([C@](C([H])([H])O[H])([H])OC1([H])O[H])O[H] | ||
| 分子式 | C6H12O5 | 分子量 | 164.16 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 20 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| 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 | 6.0916 mL | 30.4581 mL | 60.9162 mL |
| 5 mM | 1.2183 mL | 6.0916 mL | 12.1832 mL |
| 10 mM | 0.6092 mL | 3.0458 mL | 6.0916 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。
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Quality Control & SDS
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- Purity: >98.00%
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