| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | RX-3117 | ||||||||||||
| CAS | 865838-26-2 | ||||||||||||
| Formula | C10H12FN3O4 | ||||||||||||
| Molar Mass | 257.22 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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