中文名称: MS-444
英文名称: MS-444
CAS No: 150045-18-4
分子式: C13H10O4
分子量: 230.22
M10860 MS-444 ≥98% (psaitong)
包装规格:
5mg in glass bottle
溶解性:
溶于DMSO(50mg/mL 超声)
产品描述:

基本信息

产品编号:M10860

产品名称:MS-444

CAS:

150045-18-4

 

储存条件

粉末

-20℃

四年

分子式:

C19H21N3O3S

溶于液体

-80℃(避光,储存于氮)

六个月

分子量

371.45

-20℃(避光,储存于氮)

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

 

Ethanol

 

Water

 

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

4.3437mL

21.7184mL

43.4367mL

5mM

0.8687mL

4.3437mL

8.6873mL

10mM

0.4344mL

2.1718mL

4.3437mL

 

生物活性

产品描述

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

靶点/IC50

10μM (myosin)

 

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 (1-100μM) for 48 hr with IC50s of 10.98±1.76μM,12.84±2.10μM,5.60±0.90μM,14.21±2.11μM,and 10.98±1.24μM for HCT116, HCA-7, RKO, HT-29, and SW480 cells,respectively. Growth inhibition is observed in all CRC lines with IC50 values ranging from 5.60μM to 14.21μM with observable effects seen at 10μM MS-444.Contrasting effects are observed using non-transformed small intestinal (RIE-1 (IC50=40.70±3.53μM)) and colonic (YAMC (IC50=28.16±3.23μM)) 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 40.70μM and 28.16μM (P<0.05).

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 (25mg/kg bw) or vehicle every 48hr. 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.

 

推荐实验方法(仅供参考)

细胞实验:

 

Human colorectal cancer cell lines RKO, HCA-7, HCT116, HT-29,SW480 and the non-transformed intestinal epithelial cell lines RIE-1, YAMC are treated with varying concentrations of MS-444 (1-100μM) for 48 hr. Cell survival is measured by MTT assay after incubation of cells for 48 hr with MS-444. Relative cell survival is calculated as percentage normalized to DMSO vehicle-treated cells and plotted to determine IC50.

 

动物实验:

 

Mice

Athymic nude (Nu/Nu) mice are used. HCT116 (2×106 cells) and HCA-7 (2.5×106) cells resuspended in PBS are injected into the dorsal subcutaneous tissue. Mice (n=5 per group) receive intraperitoneal (IP) injections of MS-444 (25mg/kg) dissolved in PBS/5% N-Methyl Pyrrolidine (NMP) or vehicle control every 48 hr. Tumor growth is assayed.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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