|2-((2R,3R,4S,5R)-3,4-二羟基-5-(羟甲基)四氢呋喃-2-基)噻唑-4-甲酰胺|CsnPharm

CAS No.: 60084-10-8

Tiazofurin/噻唑呋林 Catalog No. CSN24086

Synonyms: NSC 286193;Riboxamide;TCAR

Tiazofurin is a synthetic nucleoside analogue with antineoplastic activity.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Inosine 5'-phosphate dehydrogenase (IMPDH) activity is increased in all cancer cells. It is the rate-limiting enzyme of guanosine triphosphate (GTP) biosynthesis, and therefore, a sensitive target of chemotherapy. Tiazofurin, a c-nucleoside, is metabolized in two enzymic steps to thiazole-4-carboxamide adenine dinucleotide (TAD), a nicotinamide adenine dinucleotide (NAD) analogue that selectively blocks IMPDH activity. Tiazofurin in vitro and in vivo potently inhibits IMPDH activity, depresses GTP and dGTP concentrations, and results in inhibition of tumor cell proliferation. The sensitivity of a particular tumor to tiazofurin depends primarily on the cellular concentration of TAD achieved. When leukemic cells are incubated with radiolabeled tiazofurin, more than a 20-fold elevation of TAD concentration is produced as compared to that achieved in bone marrow cells from healthy volunteers. Low concentrations of tiazofurin are able to induce differentiation of the human leukemic cell lines HL-60 and K-562. All these findings provide support for the use of tiazofurin for the treatment of leukemia. Institution of tiazofurin treatment in responding patients resulted in an almost instant decrease in IMPDH activity to < 10% of the pretreatment activity. The decline in GTP pools occurred more slowly, and in the majority of patients one or more dose escalations of tiazofurin were necessary to reach a > 80% decline in GTP concentrations^[1].
参考文献

[1] Tricot G, Jayaram HN, Weber G, Hoffman R. Tiazofurin: biological effects and clinical uses. Int J Cell Cloning. 1990;8(3):161‐170

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8422 mL
- 19.2110 mL
- 38.4221 mL
- 5 mM
- 0.7684 mL
- 3.8422 mL
- 7.6844 mL
- 10 mM
- 0.3842 mL
- 1.9211 mL
- 3.8422 mL

技术信息

CAS号

60084-10-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H12N2O5S

运输

蓝冰

分子量

260.27

别名

NSC 286193;Riboxamide;TCAR;噻唑呋林

溶解度

DMSO	380.0 mg/mL (1460.0 mM)
Water	310.0 mg/mL (1191.1 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Tiazofurin/噻唑呋林 Catalog No. CSN24086

靶点选择性

请登录您的专属账户

确认信息