a cytidine analog and a substrate for uridine-cytidine-kinase
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||865838-26-2||SDF||Download SDF|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
RX-3117 is a cytidine analog and a substrate for uridine-cytidine-kinase (UCK) .
Cytidine analog is activated by uridine-cytidine-kinase and is incorporated into RNA and DNA and downregulates DNA-methyltransferase-1 .
RX-3117 is a cytidine analog and inhibits DNA and RNA synthesis. In sensitive U937 cells, RX-3117 (1 μM) inhibited RNA synthesis by 90% and completely inhibited DNA synthesis. In solid tumor and leukemic cell lines, RX-3117 inhibited cell growth with IC50 values of 0.4-29.6 μM. The uptake of RX-3117 was dependent on human ENT1 (hENT). In SW1573 cells, both uridine and cytidine dose-dependently protected cells against RX-3117. RX-3117 at IC50 concentrations didn’t change the pools of both uridine and cytidine nucleotides. In three tumor cell lines, RX-3117 completely inhibited the expression of DNA-methyltransferase (DNMT). In A2780 and SW1573 cells, RX-3117 was incorporated into both RNA and DNA .
In athymic nude mice bearing Colo 205, H460, H69 and CaSki human tumor xenograft models, RX-3117 administrated orally induced tumor growth inhibition (TGI) by 100%, 78%, 62% and 66%, respectively .
. Peters GJ, Smid K, Vecchi L, et al. Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360). Invest New Drugs, 2013, 31(6): 1444-1457.
. Peters GJ. Novel developments in the use of antimetabolites. Nucleosides Nucleotides Nucleic Acids, 2014, 33(4-6): 358-374.
. Yang MY, Lee YB, Ahn CH, et al. A novel cytidine analog, RX-3117, shows potent efficacy in xenograft models, even in tumors that are resistant to gemcitabine. Anticancer Res, 2014, 34(12): 6951-6959.