Salirasib-S-Farnesylthiosalicylic-acid-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalirasibCat. No.: HY-14754CAS No.: 162520-00-5Synonyms: S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS分式: CHOS分量: 358.54作靶点: Ras; Autophagy作通路: GPCR/G Protein; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solve

2、nt -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (139.45 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.97 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.97 mM); Suspended solution

3、; Need ultrasonic3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.97 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Salirasib种 Ras 抑制剂，可特异性抑制致癌激活的Ras和长因受体介导的Ras激活，从抑制Ras依赖性肿瘤长。IC50 & Target Ki: 2.6 M (PPMTase)体外研究 Salirasib (12.5-100 M) inhibits the proliferation of ELT3 cells in a dose-depend

4、ent manner with an averageIC50 of 58.574.59 M. The effects of Salirasib on the TSC2-null cells are evidently mimicked by DN-Rhebbut not by DN-Ras. Salirasib reduces Rheb in TSC2-null cells and TSC2 expression rescues the cells fromthe inhibitory effect of Salirasib. Salirasib reduces phosphorylation

5、 of S6K but not of ERK in the TSC2-nullELT3 cells 1. Salirasib (50, 100, 150 M) induces a dose- and time-dependent decrease of cell growth inHCC cells. Salirasib reduces cell proliferation through modulation of cell cycle effectors and inhibitors.Salirasib induces apoptosis in HepG2 and Hep3B cells.

6、 The growth inhibitory effect of salirasib in HCC celllines is associated with mTOR inhibition independent of ERK or Akt activation 2.体内研究 Salirasib (40, 60 or 80 mg/kg, p.o.) significantly inhibits the tumor growth in a dose dependent manner in vivo1. Salirasib (5 mg/kg, i.p.) significantly decreas

7、es Ras expression in the dy2J/dy2Jmice, and causes anincrease 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 thedy2J/dy2J mice 2. Salirasib (10 mg/kg,

8、i.p.) inhibits tumour growth in a subcutaneous xenograft mice modelwithout weight loss 3.PROTOCOLCell Assay 3 For time dependent response studies, cells are harvested with 0.05% Trypsin-EDTA daily for 1 to 7 days andcounted under the microscope using the Trypan blue exclusion method.For dose respons

9、e studies, cells areincubated in medium supplemented with salirasib or DMSO for 3 days. Cell viability is determined using acolorimetric WST-1 assay according to the manufacturers instructions. The IC50 value, at which 50% of thecell growth is inhibited compared with DMSO control, is calculated by n

10、onlinear regression analysis usingGraphPad Prism software.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Six week old female athymic NMRI nu/nu mice are housed in filter-topped cages andreceive food and waterAdministration 3 ad libitum. Tumors a

11、re generated by subcutaneous injection into the right lower flank with 5106 HepG2 cellssuspended in 100 L PBS in 12 mice. Two weeks after cell inoculation, when palpable tumours areestablished, mice are separated into salirasib-treated (n=6) and control group (n=4). Two animals do notdevelop tumours

12、 at that time point and had to be excluded from the study. They receive daily i.p. injections of2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE10 mg/kg salirasib or a similar volume of vehicle solution (PBS containing 2.5% v/v ethanol, pH 8.0) for 12days. Tumor dimensions are recorded three times

13、per week with a digital calliper starting with the first day oftreatment. Tumor volumes are estimated as follows: V (mm3)=(lengthwidth2)/2. Tumour weights arerecorded at the time of sacrifice in order to evaluate treatment response.MCE has not independently confirmed the accuracy of these methods. T

14、hey are for reference only.户使本产品发表的科研献 Cell Death Dis. 2018 Dec 5;9(12):1170.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Makovski V, et al. Farnesylthiosalicylic acid (salirasib) inhibits Rheb in TSC2-null ELT3 cells: a potential treatment forlymphangioleiomyomatosis. Int J

15、 Cancer. 2012 Mar 15;130(6):1420-9.2. Nevo Y, et al. Chapman J. The Ras antagonist, farnesylthiosalicylic acid (FTS), decreases fibrosis and improves muscle strength indy/dy mouse model of muscular dystrophy. PLoS One. 2011 Mar 22;6(3):e18049.3. Charette N, et al. Salirasib inhibits the growth of hepatocarcinoma cell lines in vitro and tumor growth in vivo through ras and mTORinhibition. M