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Tetrahydrouridine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tetrahydrouridine图片
CAS NO:18771-50-1
包装:10 mg
市场价:2618元

产品名称
四氢尿苷
NSC112907
NSC-112907
NSC 112907
产品介绍
Tetrahydrouridine 是一种多药耐药调节剂。它可用于癌症治疗,使肿瘤细胞对放射治疗更加敏感。 它是一种竞争性胞苷脱氨酶 (CDA) 抑制剂,可抑制 ara-C 和吉西他滨等细胞毒性脱氧胞苷类似物分解代谢中的脱氨作用。

产品描述

Tetrahydrouridine (THU) is a multidrug resistance modulator. It can be used in cancer treatment to make tumor cells more sensitive to radiation therapy. THU is a competitive cytidine deaminase(CDA) inhibitor that inhibits deamination in the catabolism of cytotoxic deoxycytidine analogs such as ara-C and Gemcitabine.

体外活性

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 an 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.

体内活性

Tetrahydrouridine (167 mg/kg) followed by DAC (1.0 mg/kg) 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.

Cas No.

18771-50-1

分子式

C9H16N2O6

分子量

248.24

别名

四氢尿苷;NSC112907;NSC-112907;NSC 112907

储存和溶解度

DMSO:10mg/mL (40.29mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years