RX-3117氟环戊烯基胞嘧啶,865838-26-2

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RX-3117

CAS No. : 865838-26-2

MCE 国际站：RX-3117

产品活性：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)。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Nucleoside Antimetabolite/Analog  |  Apoptosis

In Vitro: 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.

In Vivo: RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice.

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