1. GPCR/G Protein
    Autophagy
  2. Ras
    Autophagy
  3. Salirasib

Salirasib (Synonyms: 法尼基硫代水杨酸; S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS)

目录号: HY-14754 纯度: 98.01%
产品使用指南

Salirasib是一种 Ras 抑制剂,可特异性抑制致癌激活的Ras和生长因子受体介导的Ras激活,从而抑制Ras依赖性肿瘤生长。

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Salirasib Chemical Structure

Salirasib Chemical Structure

CAS No. : 162520-00-5

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥532 In-stock
10 mg ¥484 In-stock
50 mg ¥1767 In-stock
100 mg ¥2200 In-stock
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500 mg   询价  

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查看 Ras 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.

IC50 & Target

Ki: 2.6 μM (PPMTase)

体外研究
(In Vitro)

Salirasib (12.5-100 μM) inhibits the proliferation of ELT3 cells in a dose-dependent manner with an average IC50 of 58.57±4.59 μM. 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[1]. Salirasib (50, 100, 150 μM) 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[2].

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

体内研究
(In Vivo)

Salirasib (40, 60 or 80 mg/kg, p.o.) significantly inhibits the tumor growth in a dose dependent manner in vivo[1]. Salirasib (5 mg/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[2]. Salirasib (10 mg/kg, i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss[3].

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

Clinical Trial
分子量

358.54

Formula

C₂₂H₃₀O₂S

CAS 号
中文名称

法尼基硫代水杨酸;S-法尼基硫代水杨酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (139.45 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7891 mL 13.9454 mL 27.8909 mL
5 mM 0.5578 mL 2.7891 mL 5.5782 mL
10 mM 0.2789 mL 1.3945 mL 2.7891 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: ≥ 2.5 mg/mL (6.97 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.97 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.97 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 25.0 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.97 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.97 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[3]

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.

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

Animal Administration
[3]

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 100 μL PBS in 12 mice. Two weeks after cell inoculation, when palpable tumours are established, mice are separated into salirasib-treated (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 10 mg/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.

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

参考文献

Purity: 98.72%

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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Salirasib
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HY-14754
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