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Salirasib

Chemical Structure : Salirasib

CAS No.: 162520-00-5

Salirasib (S-Farnesylthiosalicylic acid, FTS)

Catalog No.: PC-28064Not For Human Use, Lab Use Only.

Salirasib (S-Farnesylthiosalicylic acid, FTS) is an oral RAS inhibitor, shows potent competitive inhibitor of prenylated protein methyltransferase (PPMTase) with Ki of 2.6 uM, inhibits the active forms of Ras proteins.

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Biological Activity

Salirasib (S-Farnesylthiosalicylic acid, FTS) is an oral RAS inhibitor, shows potent competitive inhibitor of prenylated protein methyltransferase (PPMTase) with Ki of 2.6 uM, inhibits the active forms of Ras proteins.
Salirasib selectively inhibits growth of human Ha-ras-transformed Rat1 cells in vitro with EC50 of 7.5 uM.
Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis in Ras-transformed EJ cells.
Salirasib also inhibits MAPK activity and DNA synthesis stimulated by serum, EGF or thrombin in serum-starved untransformed Rat-1 cells.
Salirasib affects Ras membrane association but not Ras farnesylation.
Salirasib mimics c-terminal farnesyl cysteine, common to all RAS isoforms, and competes with farnesylated RAS for putative-binding sites on the plasma membrane, leading to degradation of active cytoplasmic RAS.

Physicochemical Properties

M.Wt 358.54
Formula C22H30O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(((2E,6E)-3,7,11-Trimethyldodeca-2,6,10-trien-1-yl)thio)benzoic acid

References

1. Marciano D, et al. J Med Chem. 1995 Apr 14;38(8):1267-72.

2. Marom M, et al. J Biol Chem. 1995 Sep 22;270(38):22263-70.

3. Gana-Weisz M, et al. Biochem Biophys Res Commun. 1997 Oct 29;239(3):900-4.

4. Furuse J, et al. Cancer Chemother Pharmacol. 2018 Sep;82(3):511-519.

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