Salirasib (FTS)

SKU: orb1301020

Description

Salirasib (Farnesyl Thiosalicylic Acid) is a competitive PPMTase inhibitor with a Ki of 2.6 µM, blocking Ras methylation. This activity underlies its investigated antineoplastic potential, as demonstrated in studies targeting Ras-driven cancers in both cellular and animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 162520-00-5
• MW: 358.54
• Purity: >98%
• Formula: C₂₂H₃₀O₂S
• SMILES: CC(C)=CCC\C(C)=C\CC\C(C)=C\CSc1ccccc1C(O)=O
• Target: GTPase
• Solubility: Soluble in DMSO (up to 20 mg/ml) oe in Ethanol (up to 20 mg/ml)

Bioactivity

• Target IC50:
  PPMTase:2.6 μM(Ki)
• In Vivo:
  In Panc-1 xenografted nude mice, Salirasib (5 mg/kg i.p.) markedly inhibits tumor growth without systemic toxicity. In male Wistar rats, Salirasib (5 mg/kg i.p.) markedly inhibits thioacetamide-induced -induced liver cirrhosis. In the dy(2J)/dy(2J) mouse model of congenital muscular dystrophy, Salirasib (5 mg/kg i.p.) attenuates fibrosis and improves muscle strength.
• In Vitro:
  Salirasib inhibits the growth of human Ha-ras-transformed Rat1 cells, which correlates well with their inhibition for PPMTase. Salirasib inhibits Ras methylation in Rat-1 fibroblasts, Ras-transformed Rat-1, and B16 melanoma cells. Salirasib also reduces the levels of Ras in cell membranes and inhibits Ras-dependent cell growth, independently of methylation, but via modulation of Ras-Raf communication. In Ras-transformed EJ cells, Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis.
• Cell Research:
  Cells are grown in 24-well plates. 2 h after plating, the cells receive either solvent or FTS freshly prepared from a stock solution to yield the final indicated concentrations in 0.1% DMSO. Media are replaced every 4 days with fresh medium containing the solvent or the drug. Separate experiments indicate that the solvent itself has no effect on cell growth. On the indicated days, the cells are detached from plates by trypsin/EDTA and counted under the light microscope. All assays are performed in quadruplicate. In parallel experiments, cells are stained either with trypan blue or with MTT, and the stained cells are examined under the light microscope. In some MTT-stained cultures, the cells are dissolved in 0.2 mL of 100% DMSO, and the extent of staining is determined spectrophotometrically using an enzyme-linked immunosorbent assay reader.(Only for Reference)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, FTS, Farnesyl Thiosalicylic Acid, Inhibitor, inhibit, Ras, S-Farnesylthiosalicylic acid, PPMTase, Salirasib

Compound Identifiers

PubChem CID

5469318