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RX-3117
a cytidine analog and a substrate for uridine-cytidine-kinase

RX-3117

Catalog No. B5828
Size Price Stock
5mg Please Inquire Please Inquire
25mg Please Inquire Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

RX-3117

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Chemical Properties

Cas No. 865838-26-2 SDF Download SDF
Chemical Name (1S,2R,5S)-4-fluoro-5-(2-hydroxy-4-iminopyrimidin-1(4H)-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol
Canonical SMILES FC([C@](N(C(O)=N1)C=CC1=N)([H])[C@@](O)([H])[C@]2([H])O)=C2CO
Formula C10H12FN3O4 M.Wt 257.22
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

RX-3117 is a cytidine analog and a substrate for uridine-cytidine-kinase (UCK) [1].

Cytidine analog is activated by uridine-cytidine-kinase and is incorporated into RNA and DNA and downregulates DNA-methyltransferase-1 [2].

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 [1].

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 [3].

References:
[1].  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.
[2].  Peters GJ. Novel developments in the use of antimetabolites. Nucleosides Nucleotides Nucleic Acids, 2014, 33(4-6): 358-374.
[3].  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.