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Salirasib | Ras inhibitor

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

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Salirasib | 162520-00-5 | Structure | Supplier

Catalog#  10-1461

$30.00
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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.
 
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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:
Room temperature (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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