MS-444 BE-34776|cas:150045-18-4|西域试剂

MS-444 BE-34776,98.09%

产品编号：Bellancom-100685| CAS NO：150045-18-4| 分子式：C₁₃H₁₀O₄| 分子量：230.22

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-100685		￥6200.00	杭州北京（现货）
Bellancom-100685		￥9800.00	杭州北京（现货）

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MS-444 BE-34776

产品介绍

MS-444 是平滑肌肌球蛋白轻链激酶 (MLCK) 的抑制剂，IC₅₀ 值为 10 μM。

生物活性

MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC₅₀ value of 10 μM.

体外研究

MS-444 is a small molecule RNA-binding protein HuR (ELAVL1) inhibitor. Colorectal cancer (CRC) cells that display HuR overexpression are treated with MS-444 (1-100 μM) for 48 hr with IC₅₀s of 10.98±1.76 μM, 12.84±2.10 μM, 5.60±0.90 μM, 14.21±2.11 μM, and 10.98±1.24 μM for HCT116, HCA-7, RKO, HT-29, and SW480 cells, respectively. Growth inhibition is observed in all CRC lines with IC₅₀ values ranging from 5.60 μM to 14.21 μM with observable effects seen at 10 μM MS-444. Contrasting effects are observed using non-transformed small intestinal (RIE-1 (IC₅₀=40.70±3.53 μM)) and colonic (YAMC (IC₅₀=28.16±3.23 μM)) epithelial cells. Both cell types display properties of normal intestinal epithelial cells and are proficient in 3′UTR AU-rich elements (ARE)-mRNA decay. Both non-transformed cell lines are ~3- to 4-fold less responsive to MS-444-mediated growth inhibition, with IC₅₀ values of 40.70 μM and 28.16 μM (P<0.05).

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

体内研究

To test the effects of MS-444 on CRC cell growth in vivo, mice bearing HCT116 cell xenografts receive IP injections of MS-444 (25 mg/kg bw) or vehicle every 48 hr. Over the experiment course, mice do not display any adverse effects and maintained similar weights. Anti-tumor effects of MS-444 are observed with approximately 1.7-fold reduction in tumor size. Mice treated with MS-444 show a marked 2- to 3-fold decrease in microvessel density (MVD), indicating the anti-angiogenic potential of MS-444.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (217.18 mM; Need ultrasonic)

1-Methyl-2-pyrrolidinone : 20 mg/mL (86.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3437 mL	21.7184 mL	43.4367 mL
5 mM	0.8687 mL	4.3437 mL	8.6873 mL
10 mM	0.4344 mL	2.1718 mL	4.3437 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 (protect from light, stored under nitrogen)。-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% 1-Methyl-2-pyrrolidinone 90% PBS
Solubility: 2 mg/mL (8.69 mM); Suspended solution; Need ultrasonic and warming and heat to 50°C
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2 mg/mL (8.69 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (8.69 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 20.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (8.69 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (8.69 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明