Salirasib - CAS:162520-00-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Salirasib
英文名称:	Salirasib
别名:	法尼基硫代水杨酸 2-(((2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrienyl)sulfanyl)benzoic acid
CAS No:	162520-00-5	分子式:	C₂₂H₃₀O₂S	分子量:	358.54
CAS No:	162520-00-5
分子式:	C₂₂H₃₀O₂S
分子量:	358.54
MDL:	MFCD00467723

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S10052 Salirasib ≥98% (HPLC) (psaitong)

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包装规格：

50mg 100mg in glass bottle

溶解性：

溶于DMSO( 20mg/mL)

产品描述：

基本信息

产品编号：	S10052
产品名称：	Salirasib
CAS:	162520-00-5	储存条件	粉末	-20℃	四年

分子式：	C22H30O2S		溶于液体	-80℃	6个月
分子量：	358.54			-20℃	1个月
化学名：	2-(((2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrienyl)sulfanyl)benzoic acid
Solubility (25°C)：
体外:	DMSO	72mg/mL (200.81mM)
	Ethanol	72mg/mL (200.81mM)
	Water	Insoluble
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	2.7891mL	13.9454mL	27.8909mL
5mM	0.5578mL	2.7891mL	5.5782mL
10mM	0.2789mL	1.3945mL	2.7891mL
50mM	0.0558mL	0.2789mL	0.5578mL

生物活性

产品描述	一种具有潜在抗肿瘤活性的水杨酸衍生物,是有效的PPMTase抑制剂，Ki：2.6μM；也可抑制Ras甲基化。
靶点	Ras	PPMTase
		2.6μM(Ki)
体外研究	Salirasib (12.5-100μM) inhibits the proliferation of ELT3 cells in a dose-dependent manner with an average IC50 of 58.57±4.59μM.The effects of Salirasib on the TSC2-null cells are evidently mimicked by DN-Rheb but not by DN-Ras.Salirasib reduces Rheb in TSC2-null cells and TSC2 expression rescues the cells from the inhibitory effect of Salirasib.Salirasib reduces phosphorylation of S6K but not of ERK in the TSC2-null ELT3 cells.Salirasib (50,100,150μM) induces a dose- and time-dependent decrease of cell growth in HCC cells.Salirasib reduces cell proliferation through modulation of cell cycle effectors and inhibitors. Salirasib induces apoptosis in HepG2 and Hep3B cells. The growth inhibitory effect of salirasib in HCC cell lines is associated with mTOR inhibition independent of ERK or Akt activation.
体内研究	Salirasib (40,60 or 80mg/kg,p.o.) significantly inhibits the tumor growth in a dose dependent manner in vivo.Salirasib (5mg/kg,i.p.) significantly decreases Ras expression in the dy2J/dy2Jmice,and causes an increase in Ras expression which is by far much lower than the increase observed in the dy2J/dy2J mice.Salirasib treatment is associated with significantly inhibition of both MMP-2 and MMP-9 activities in the dy2J/dy2J mice.Salirasib (10mg/kg,i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss.

推荐实验方法(仅供参考)

激酶实验：

PPMTase 试验

大鼠小脑突触体膜或培养细胞系的总膜(100,000×g 沉淀)用于无细胞体系中甲基转移酶测定。甲基转移酶在总体积为50μL 的50mM Tris-HCl 缓冲液中，pH 7.4，使用100μg蛋白质，25 μM [methyl-3H]AdoMet (300,000 cpm/nmol)，和50μM AFC (在DMSO中以原液制备)，于37°C下进行测定。所有试验的DMSO浓度为8%。不同AFC浓度按照指示用于各实验中。加入500μL氯仿：甲醇 (1:1) 10分钟后，终止反应，随后加入250μL H2O，混合，并相分离。氯仿相的125-μL部分在40℃下干燥，并加入200μl 的1 N NaOH和1% SDS溶液。因此形成的甲醇通过气相平衡法计算。典型的背景计数(无AFC 添加)为50-100 cpm，而与AFC的典型反应产生500-6,000 cpm。试验以一式三份进行，减去背景计数。使内源性底物甲基化，并进行凝胶电泳。完整细胞中的蛋白质羧基甲基化使用100μCi/mL [methyl-3H]甲硫氨酸测定。细胞近似铺满培养基，在含有5mL 标记培养基的10-cm板中生长测定。

细胞实验:

For time dependent response studies,cells are harvested with 0.05% Trypsin-EDTA daily for 1 to 7 days and counted under the microscope using the Trypan blue exclusion method.For dose response studies,cells are incubated in medium supplemented with salirasib or DMSO for 3 days.Cell viability is determined using a colorimetric WST-1 assay according to the manufacturer's instructions.The IC50 value,at which 50% of the cell growth is inhibited compared with DMSO control, is calculated by nonlinear regression analysis using GraphPad Prism software.

动物实验:

Six week old female athymic NMRI nu/nu mice are housed in filter-topped cages andreceive food and water ad libitum.Tumors are generated by subcutaneous injection into the right lower flank with 5×106 HepG2 cells suspended in 100μL PBS in 12 mice.Two weeks after cell inoculation,when palpable tumours are established,mice are separated into salirasibtreated (n=6) and control group (n=4).Two animals do not develop tumours at that time point and had to be excluded from the study.They receive daily i.p.injections of 10mg/kg salirasib or a similar volume of vehicle solution (PBS containing 2.5% v/v ethanol,pH 8.0) for 12 days.Tumor dimensions are recorded three times per week with a digital calliper starting with the first day of treatment.Tumor volumes are estimated as follows:V (mm3)=(length×width2)/2.Tumour weights are recorded at the time of sacrifice in order to evaluate treatment response.

保存条件：

-20℃

UN码：

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