产品名称

替莫唑胺(Temozolomide)

一般描述

Temozolomide(替莫唑胺) is a triazene analog of dacarbazine with antineoplastic activity.

别 称

3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide; NSC 362856

纯 度

≥99%(HPLC)

CAS NO.

85622-93-1

分子式

C⁶H⁶N⁶O²

分子量

194.15

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

浅紫色或棕色固体

溶解性(25℃)

DMSO

≥35mg/mL

乙醇

Insoluble

水

Slightly  soluble

l  生物学信息

生物活性/药理作用

Temozolomide is an imidazotetrazine deritave and an antineoplastic agent. It is a prodrug that has little to no pharmacological activity until it is hydrolyzed in vivo to 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC). After administration, temozolomide undergoes rapid, nonenzymatic hydrolysis at physiological pH to MTIC, which is the active form of the drug. MTIC is generated through the effect of water at the highly electropositive C4 position of temozolomide, causing the ring of temozolomide to open, release carbon dioxide, and generate MTIC.

Temozolomide is a triazene analog of dacarbazine with antineoplastic activity. As a cytotoxic alkylating agent, temozolomide is converted at physiologic pH to the short-lived active compound, monomethyl triazeno imidazole carboxamide (MTIC). The cytotoxicity of MTIC is due primarily to methylation of DNA at the O6 and N7 positions of guanine, resulting in inhibition of DNA replication. Unlike dacarbazine, which is metabolized to MITC only in the liver, temozolomide is metabolized  to MITC at all sites. Temozolomide is administered orally and penetrates well  into the central nervous system.

l  包装与存储

包 装

50mg; 1g

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov