您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Raltitrexed
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Raltitrexed
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。
Raltitrexed图片
CAS NO:112887-68-0
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
ZD1694
雷替曲塞
D1694
ICI-D1694
Tomudex
产品介绍
Raltitrexed是一种抗代谢药物,通过抑制胸苷酸合成酶起作用,可用于化疗。

产品描述

Raltitrexed(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.

体外活性

Raltitrexed induces double-stranded DNA breaks in a concentration-dependent manner. In Lovo cells and LS174T cell lines containing wild-type p53, Raltitrexed increases the levels of the Bax protein up to 5-fold. In human colon cancer cells, Raltitrexed is actively absorbed into cells and is then rapidly and extensively metabolized into a series of polyglutamates, which results in the effective inhibition of thymidylate synthase. Raltitrexed is delivered to the brain very quickly and can be detected in all brain tissues within 5 minutes. In human colon cancer cells, the combination of Raltitrexed and SN-38 results in a synergistic cytotoxic effect within a range of concentrations. Raltitrexed is a specific folate-based inhibitor of thymidylate synthase. The effect on the activity of advanced rectal cancer is similar to fluorouracil (5-fluorouracil) plus leucovorin. Raltitrexed produces activity by rapid cell entry and glutamination. The glutaminated derivatives are more than 100 times more active than the parent compound. In the HCT-8 cell line, Raltitrexed results in an increase in intracellular phosphoribosyl pyrophosphate (PRPD) indicating that the cytotoxic effect of Raltitrexed in combination with 5-FU is due to increased nucleotide formation of 5-FU. Combinations of Raltitrexed and folinic acid (5FU-FA) show a combination of mode-dependent, synergistic inhibition of proliferation, which is determined by measuring the combination series. Raltitrexed combined with Vorinostat produced significant synergistic effects of cell cycle perturbation and S-phase arrest.

体内活性

Raltitrexed can be transported directly into the brain through the olfactory pathway in rats.

Cas No.

112887-68-0

分子式

C21H22N4O6S

分子量

458.49

别名

ZD1694;雷替曲塞;D1694;ICI-D1694;Tomudex

储存和溶解度

H2O:<1 mgml
DMSO:84 mg/mL (183.2 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years