RX-3117 (TV-1360) 是一种有效的口服活性抗癌和抗代谢物药剂。RX-3117 抑制 DNA 甲基转移酶 1 (DNMT1。RX-3117 显示出抗增殖和抗肿瘤活性。RX-3117 诱导细胞周期停滞在 S 期和细胞凋亡 (apoptosis)。
| 生物活性 | RX-3117 (TV-1360) is a potent and orally activeanticancerandantimetaboliteagent. RX-3117 inhibitsDNA methyltransferase1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase andapoptosis[1][2][3]. |
体外研究
(In Vitro) | 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: | 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 Analysis[2] | Cell 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. |
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体内研究
(In Vivo) | RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice[3].
| Animal Model: | Nude mice (human colon carcinoma HCT116 xenograft model)[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(194.39 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.8877 mL | 19.4386 mL | 38.8772 mL | | 5 mM | 0.7775 mL | 3.8877 mL | 7.7754 mL | | 10 mM | 0.3888 mL | 1.9439 mL | 3.8877 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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