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RX-3117
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。
RX-3117图片
CAS NO:865838-26-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
fluorocyclopentenylcytosine
TV-1360
产品介绍
RX-3117 是一种新型的胞苷类似物,在几种癌细胞系中显示出抗癌活性,包括对吉西他滨耐药的变体。

产品描述

RX-3117 is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

体外活性

RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine and azacytidine, substrates for uridine-cytidine-kinase. Insensitive U937 cells 1 μM RX-3117 resulted in 90% inhibition of RNA synthesis but 100 μM RX-3117 was required in A2780 and CCRF-CEM cells. RX-3117 at IC50 values did not affect the integrity of RNA [1].

体内活性

RX-3117 (p.o.) was examined in 9 different human tumor xenograft models grown subcutaneously in athymic nude mice. In the Colo 205, H460, H69 and CaSki models, gemcitabine treatment resulted in 28%, 30%, 25% and 0% tumor growth inhibition (TGI), respectively. Whereas oral treatment with RX-3117 induced 100%, 78%, 62% and 66% TGI, respectively [2].

Cas No.

865838-26-2

分子式

C10H12FN3O4

分子量

257.22

别名

fluorocyclopentenylcytosine;TV-1360

储存和溶解度

DMSO:50 mg/mL (194.39 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years