[CAS NO. 162520-00-5] Salirasib

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PRODUCTS SPECIFICATIONS [162520-00-5]

Catelog

SLK-S7684

Brand

Selleck

CAS

162520-00-5

DESCRIPTION [162520-00-5]

Overview

MDL	MFCD00467723
Molecular Weight	358.54
Molecular Formula	C22H30O2S
SMILES	S(C/C=C(/CC/C=C(/CCC=C(C)C)\C)\C)C1=C(C(O)=O)C=CC=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive inhibitor with K of 2.6 μM, which inhibits methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.

Targets

Ras ^[1]	PPMTase ^[1]
	2.6 μM(Ki)

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.

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.

References

[1] Marciano D, et al. J Med Chem. 1995, 38(8), 1267-1272.
[2] Marom M, et al. J Biol Chem. 1995, 270(38), 22263-22270.
[3] Gana-Weisz M, et al. Biochem Biophys Res Commun. 1997, 900-904.
[4] Weisz B, et al. Oncogene. 1999, 18(16), 2579-2588.
[5] Reif S, et al. J Hepatol. 1999, 31(6),, 1053-1061.
[6] Nevo Y, et al. PLoS One. 2011, 6(3), e18049.

Synonyms

Benzoic acid, 2-[[(2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrien-1-yl]thio]-

Benzoic acid, 2-[(3,7,11-trimethyl-2,6,10-dodecatrienyl)thio]-, (E,E)-

Benzoic acid, 2-[[(2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrienyl]thio]-

2-[[(2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrien-1-yl]thio]benzoic acid

S-Farnesylthiosalicylic acid

FTS

Salirasib

Farnesylthiosalicylic acid