For research use only. Not for therapeutic Use.
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis[1][2][3].
RX-3117 causes both inhibition of DNA and RNA synthesis[1].
RX-3117 (11.7, 21 μM; 48 h) shows antiproliferative activity in A549, SW1573 cells[1].
RX-3117 is activated by uridine-cytidine kinase 2 (UCK2)[1].
RX-3117 (1-25 μM; 72 h) inhibits the growth of HCT-116, MDA-MB-231, PANC-1, Caki-1, MCF7, A549, MKN45, U251 cells with IC50s of 0.39, 0.18, 0.62, 0.84, 0.34, 0.34, 0.50, 0.83 μM, respectively[2].
RX-3117 (5, 10 μM; 4 days) induces cell cycle arrest at S phase and apoptosis[2].
RX-3117 (1-5 μM; 24 h) decreases the cellular amount of DNMT1 in a dose-dependent manner in MDA-MB-231[3].
RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice[3].
| Catalog Number | I005207 |
| CAS Number | 865838-26-2 |
| Synonyms | 4-amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl]pyrimidin-2-one |
| Molecular Formula | C10H12FN3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C10H12FN3O4/c11-6-4(3-15)8(16)9(17)7(6)14-2-1-5(12)13-10(14)18/h1-2,7-9,15-17H,3H2,(H2,12,13,18)/t7-,8-,9+/m1/s1 |
| InChIKey | QLLGKCJUPWYJON-HLTSFMKQSA-N |
| SMILES | C1=CN(C(=O)N=C1N)C2C(C(C(=C2F)CO)O)O |
| Reference | [1]. Sarkisjan D, et al. The Cytidine Analog Fluorocyclopentenylcytosine (RX-3117) Is Activated by Uridine-Cytidine Kinase 2. PLoS One. 2016 Sep 9;11(9):e0162901. [2]. Balboni B, et al. RX-3117 (fluorocyclopentenyl cytosine): a novel specific antimetabolite for selective cancer treatment. Expert Opin Investig Drugs. 2019 Apr;28(4):311-322. [3]. Fahy J, et al. DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies. Expert Opin Ther Pat. 2012 Dec;22(12):1427-42. |
