产品名称

Evofosfamide (TH-302)

一般描述

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.

别 称

Evofosfamide; 2-bromo-N-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine

纯 度

≥98.0%(HPLC)

CAS NO.

918633-87-1

分子式

C⁹H¹⁶Br²N⁵O⁴P

分子量

449.04

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

≥5mg/mL

l  生物学信息

生物活性/药理作用

Evofosfamide is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM) conjugated with 2-nitroimidazole, with potential antineoplastic activity. When exposed to  hypoxic conditions, such as those found in hypoxic tumors, the 2-nitroimidazole moiety of evofosfamide is reduced. This releases the  DNA-alkylating Br-IPM moiety, which introduces intra- and inter-strand DNA crosss in nearby cells; the crosss inhibit both DNA replication and cell division, and may lead to apoptosis of cells in the tumor. The inactive form of the prodrug is stable under normoxic conditions, which may limit systemic toxicity.

l  存储

存储温度

-20°C

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