| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89183-5mg促销 |
99.80% | ￥270.00 ￥216.00 |
5 | - | - | - | - |
|
S89183-10mg促销 |
99.80% | ￥500.00 ￥400.00 |
6 | - | - | - | - |
|
S89183-25mg促销 |
99.80% | ￥850.00 ￥680.00 |
5 | - | - | - | - |
|
S89183-100mg促销 |
≥98% | ￥2450.00 ￥1960.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models | ||||||||||||||||||||
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| 靶点： | Perinucleolar compartment;DNA/RNASynthesis | ||||||||||||||||||||
| 体外研究： | 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 | ||||||||||||||||||||
| 体内研究： | 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. Animal Model: NOD/IL2 gamma (null) PANC1 mice over primary tumor tissues Dosage: 5 and 25 mg/kg Administration: IP; once daily; continuing for six weeks Result: Displayed a decrease in metastatic burden in both liver (p <0.01) and lung with 25 mg/kg.Demonstrated a significant reduction of perinucleolar compartment prevalence in metastatic and primary tumor tissues. Animal Model: Female BALB/c mice Dosage: 5 and 25 mg/kg (Pharmacokinetic Analysis) Administration: IP Result: Indicated good exposure, distribution, and tolerability in vivo, with a half-life of 4.6 to 5.5 hours. | ||||||||||||||||||||
| 动物实验： | Metarrestin (ML246) is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models. | ||||||||||||||||||||
| 参考文献： | 1. Vilimas T, et al. Pharmacokinetic evaluation of the perinucleolar compartment disassembler metarrestin in wild-type and Pdx1-Cre;LSL-KrasG12D/+;Tp53R172H/+ (KPC) mice, a genetically engineered model of pancreatic cancer. Cancer Chemother Pharmacol. 2018 D 2. Frankowski KJ, et al. Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis. Sci Transl Med. 2018 May 16;10(441). | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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