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Metarrestin

CAS No. : 1443414-10-5

MCE 站：Metarrestin

产品活性：Metarrestin (ML246) 是一种口服有效的，首创的，选择性的核周区室 (PNC) 抑制剂。Metarrestin 破坏核仁结构并抑制 RNA 聚合酶 (Pol) I 转录，部分是由于与翻译延伸因子 eEF1A2 的相互作用。Metarrestin 可以阻断小鼠癌症模型的转移发展，并延长存活期。

研究领域：Cell Cycle/DNA Damage

作用靶点：DNA/RNA Synthesis

In Vitro: Metarrestin (ML246) disrupts perinucleolar compartments in PC3M-GFP-PTB cells with an IC₅₀ of 0.39 μM.
Metarrestin (1 μM; 24 hours) reduces perinucleolar compartment prevalence in different human cancer cell lines. Metarrestin impacts cell growth in cancer cell line PC3M but not in normal fibroblasts (GM02153).
Metarrestin (0.6 μM; 24 hours) effectively blocks the invasion of PC3M and PANC1 cells.
Metarrestin (1 μM; 24 hours) does not significantly change the amounts of Pol I large subunit RPA194 and UBF in the three cell lines, PANC1, PC3M, and HeLa. Metarrestin shows a substantial reduction of 5’ETS RNA in cells.

In Vivo: Metarrestin (ML246; 5-25 mg/kg; IP; once daily; continuing for six weeks) displays a decrease in metastatic burden in both liver (p <0.01) and lung with 25 mg/kg.
Metarrestin (drug-infused chow; 10 mg/kg; 70 ppm) extends survival in the NSG PANC1 pancreatic cancer metastasis mice model.
Metarrestin (5, 25 mg/kg; ip; for 4 additional week) reduces metastasis of prostate cancer (PC3M) and growth of metastatic breast cancer PDX mice models.
Metarrestin (5 and 25 mg/kg; IP) has a half-life of 4.6 to 5.5 hours.

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