RX-3117

RX-3117 (TV-1360) is a potent and orally active anticancer and antimetabolite agent. 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 .In VitroRX-3117 causes both inhibition of DNA and RNA synthesis. ?\nRX-3117 (11.7, 21 μM; 48 h) shows antiproliferative activity in A549, SW1573 cells. ?\nRX-3117 is activated by uridine-cytidine kinase 2 (UCK2). ?\nRX-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 IC 50 s of 0.39, 0.18, 0.62, 0.84, 0.34, 0.34, 0.50, 0.83 μM, respectively. ?\nRX-3117 (5, 10 μM; 4 days) induces cell cycle arrest at S phase and apoptosis. ?\nRX-3117 (1-5 μM; 24 h) decreases the cellular amount of DNMT1 in a dose-dependent manner in MDA-MB-231. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549, SW1573 cells Concentration: 11.7, 21 µM Incubation Time: 48 h Result: Showed antiproliferative activity in A549 (63.7% cell growth), SW1573 cells (59% cell growth). Apoptosis AnalysisCell Line: A549, SW1573 NSCLC cells Concentration: 5 µM for A549 cells, 10 µM for SW1573 cells Incubation Time: 4 days Result: Induced cell cycle arrest at S phase and apoptosis.In VivoRX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (human colon carcinoma HCT116 xenograft model)Dosage: 2, 10 mg/kg Administration: I.p.; three times per week for five weeks Result: Caused significant inhibition of tumor growth at the doses of 2 and 10 mg/kg.Form:Solid

Specifictaions: Moligand™, ≥98%

MDL Number: C10H12FN3O4

Molecular Formula: 257.22

PubChem CID: 11242315

Isomeric SMILES: C1=CN(C(=O)N=C1N)[C@H]2[C@@H]([C@@H](C(=C2F)CO)O)O