Salirasib  (Synonyms: S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS)

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.

Ki: 2.6 μM (PPMTase)

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].

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

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 dy^2J/dy^2Jmice, and causes an increase in Ras expression which is by far much lower than the increase observed in the dy^2J/dy^2J mice. Salirasib treatment is associated with significantly inhibition of both MMP-2 and MMP-9 activities in the dy^2J/dy^2J mice^[2]. Salirasib (10 mg/kg, i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss^[3].

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

358.54

C₂₂H₃₀O₂S

162520-00-5

Solid

White to light yellow

O=C(O)C1=CC=CC=C1SC/C=C(C)/CC/C=C(C)/CC/C=C(C)/C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Makovski V, et al. Farnesylthiosalicylic acid (salirasib) inhibits Rheb in TSC2-null ELT3 cells: a potential treatment for lymphangioleiomyomatosis. Int J Cancer. 2012 Mar 15;130(6):1420-9.  [Content Brief]

  [2]. Nevo Y, et al. Chapman J. The Ras antagonist, farnesylthiosalicylic acid (FTS), decreases fibrosis and improves muscle strength in dy/dy mouse model of muscular dystrophy. PLoS One. 2011 Mar 22;6(3):e18049.  [Content Brief]

  [3]. Charette N, et al. Salirasib inhibits the growth of hepatocarcinoma cell lines in vitro and tumor growth in vivo through ras and mTOR inhibition. Mol Cancer. 2010 Sep 22;9:256.  [Content Brief]