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)。

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.

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RX-3117 causes both inhibition of DNA and RNA synthesis.
RX-3117 (11.7, 21 μM; 48 h) shows antiproliferative activity in A549, SW1573 cells.
RX-3117 is activated by uridine-cytidine kinase 2 (UCK2).
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.
RX-3117 (5, 10 μM; 4 days) induces cell cycle arrest at S phase and apoptosis.
RX-3117 (1-5 μM; 24 h) decreases the cellular amount of DNMT1 in a dose-dependent manner in MDA-MB-231. has not independently confirmed the accuracy of these methods. They are for reference only.

RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (human colon carcin

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[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.

In Vitro: DMSO : ≥ 50 mg/mL (194.39 mM)配制储备液