Metarrestin ML246|cas:1443414-10-5|西域试剂

Metarrestin ML246,99.96%

产品编号：Bellancom-120118| CAS NO：1443414-10-5| 分子式：C₃₁H₃₀N₄O| 分子量：474.60

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货号	价格	库存与货期
Bellancom-120118	￥1700.00	杭州北京（现货）
Bellancom-120118	￥2900.00	杭州北京（现货）
Bellancom-120118	￥5800.00	杭州北京（现货）
Bellancom-120118	￥9900.00	杭州北京（现货）
Bellancom-120118	￥0.00	杭州北京（现货）

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Metarrestin ML246

产品介绍

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。

生物活性

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (65.84 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1070 mL	10.5352 mL	21.0704 mL
5 mM	0.4214 mL	2.1070 mL	4.2141 mL
10 mM	0.2107 mL	1.0535 mL	2.1070 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (4.38 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.38 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液