Tetrahydrouridine dihydrate
(Synonyms: 四氢尿苷; THU dihydrate; NSC-112907 dihydrate) 目录号 : GC61326
Tetrahydrouridinedihydrate(THUdihydrate)是一种有效的胞苷脱氨酶(CDA)抑制剂,竞争性阻断酶的活性位点。
Sample solution is provided at 25 µL, 10mM.
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
Tetrahydrouridine (THU) is a specific inhibitor of cytidine deaminase (CDA) which can suppress deamination in the catabolism of cytotoxic deoxycytidine analogues like ara-C and Gemcitabine. To test how Tetrahydrouridine affects the Gemcitabine-mediated anti-neoplastic effect on pancreatic and lung carcinoma cells, a combination therapy is performed. As expected, high CDA expression in BxPC-3 and H441 results in improved Gemcitabine sensitivity after a 100 µM Tetrahydrouridine treatment. The sensitivity of BxPC-3 and H441 cell lines increases by as much as approximately 2.1 and 4.4 fold respectively. On the other hand, MIAPaCa-2 and H1299 cells unexpectedly become more sensitive to Gemcitabine with low CDA expression. MIAPaCa-2 and H1299 cells show a change in IC50 of 2.2 and 2.3 fold respectively. However, Panc-1 and H322 cells do not show significant changes in drug sensitivity. These data suggested that Tetrahydrouridine can sensitize some pancreatic and lung carcinoma cells to Gemcitabine-induced cell death regardless of CDA expression levels. Tetrahydrouridine inhibits S-phase without apoptosis[1].
Administration of 167 mg/kg Tetrahydrouridine (THU) followed by 1.0 mg/kg DAC results in death in one male and eight females. Animals surviving to scheduled termination are generally asymptomatic with no treatment related effects observed in body weights, food consumption, clinical chemistry and urinalysis for a treatment up to 1.0 mg/kg DAC in combination with 167 mg/kg Tetrahydrouridine in animals[2].
[1]. Funamizu N, et al. Tetrahydrouridine inhibits cell proliferation through cell cycle regulation regardless of cytidine deaminase expression levels. PLoS One. 2012;7(5):e37424. [2]. Terse P, et al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85.
Cas No. | SDF | ||
别名 | 四氢尿苷; THU dihydrate; NSC-112907 dihydrate | ||
Canonical SMILES | O=C1N([C@H]2[C@H](O)[C@H](O)[C@@H](CO)O2)CCC(O)N1.[H]O[H].[H]O[H] | ||
分子式 | C9H20N2O8 | 分子量 | 284.26 |
溶解度 | DMSO: ≥ 100 mg/mL (351.79 mM); Water: 50 mg/mL (175.90 mM) | 储存条件 | Solution, -20°C, 2 years |
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1 mg | 5 mg | 10 mg |
1 mM | 3.5179 mL | 17.5895 mL | 35.1791 mL |
5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL |
10 mM | 0.3518 mL | 1.759 mL | 3.5179 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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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- Purity: >85.00%
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