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