Salirasib | Ras inhibitor

CAS:
162520-00-5
Catalog Number:
10-1461
Activity:
Ras inhibitor
Chemical Name:
trans-Farnesylthiosalicylic acid
Molecular Weight:
358.54
Molecular Formula:
C22H30O2S
Solubility:
Soluble in DMSO (up to 20 mg/ml) oe in Ethanol (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$35.00
25 mg$140.00

Salirasib (162520-00-5) is a synthetic farnesylcysteine mimetic that inhibits ras proteins1,2 via disruption of interactions between the S-Prenyl moiety of Ras and the membrane anchorage domains3.  It has been investigated in the treatment of various cancers.4,5  HCC cells pretreated with salirasib were sensitized to TRAIL-induced apoptosis.6 Salirasib has also been shown to inhibit TRPA1 (EC50 = 1.3 μM).7

References/Citations:

1) Marciano et al. (1995), Farnesyl Derivatives of Rigid Carboxylic Acids – Inhibitors of ras-Dependent Cell Growth; J. Med. Chem., 38 1267
2) Marom et al. (1995), Selective inhibition of Ras-dependent cell growth by farnesylthiosalicylic acid (salirasib) in patients with solid tumors; J. Biol. Chem., 270 22263
3) Haklai et al. (1998), Dislodgement and Accelerated Degradation of Ras; Biochemistry, 37 1306
4) Laheru et al. (2012), Integrated preclinical and clinical development of S-trans,trans-Farnesylthiosalicylic acid (FTS, Salirasib) in pancreatic cancer; Invest .New Drugs, 30 2391
5) Tsimberidou et al. (2010), Phase 1 first-in-human clinical study of S-trans,trans-farnesylthiosalicylic acid (salirasib) in patients with solid tumors; Cancer Chemother. Pharmacol., 65 235
6) Charette et al. (2013), Salirasib sensitizes hepatocarcinoma cells to TRAIL-induced apoptosis through DR5 and survivin-dependent mechanisms; Cell Death and Disease. 4 e471
7) Maher et al. (2008), Activation of TRPA1 by farnesyl thiosalicylic acid; Mol. Pharmacol., 73 1225

CAS:
162520-00-5
Catalog Number:
10-1461
Activity:
Ras inhibitor
Chemical Name:
trans-Farnesylthiosalicylic acid
Molecular Weight:
358.54
Molecular Formula:
C22H30O2S
Solubility:
Soluble in DMSO (up to 20 mg/ml) oe in Ethanol (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee