162520-00-5 Usage
Description
Salirasib, also known as Farnesyl thiosalicylic acid (FTS), is a new specific nontoxic drug with a mild hydrophobic nature. It acts as a Ras antagonist, which is crucial for the association of Ras protein with the inner surface of the plasma membrane, a requirement for Ras signaling activity. By dislodging Ras from the cell membrane, Salirasib renders it susceptible to proteolytic degradation, thus inhibiting Ras-mediated signaling.
Uses
Used in Stent Applications:
Salirasib is used as a Ras antagonist for stent applications, where its ability to inhibit Ras signaling can help prevent the development of atherosclerotic lesions and improve the effectiveness of stent placement.
Used in Local Cancer Treatment:
In the field of oncology, Salirasib is used as a farnesyltransferase inhibitor for local cancer treatment. It has been shown to inhibit the growth of human Ha-ras-transformed Rat1 fibroblasts and can be used in combination with other treatments to enhance the efficacy of cancer therapy.
Used in Atherosclerosis Treatment:
Salirasib has been used as a treatment for atherosclerosis, demonstrating a significant reduction in early atherosclerotic lesion development when administered to ApoE-deficient mice. Its ability to inhibit Ras signaling and prenylated protein methyltransferase (PPMTase) makes it a promising candidate for further research and development in this area.
Chemical Properties:
Salirasib is a pale yellow solid, which contributes to its mild hydrophobic nature and its potential for use in various pharmaceutical applications.
Biochem/physiol Actions
Salirasib (Farnesylthiosalicylic acid) is a RAS inhibitor that acts by dislodging the farnesylated protein from the membrane, facilitating Ras degradation. Salirasib impairs downstream signaling and suppresses growth and migration of proliferating tumor cells in in vitro and in vivo models. Salirasib (Farnesylthiosalicylic acid) has recently been shown to possess significant anti-inflammatory and anti-arthritic properties.
References
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
Check Digit Verification of cas no
The CAS Registry Mumber 162520-00-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,2,5,2 and 0 respectively; the second part has 2 digits, 0 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 162520-00:
(8*1)+(7*6)+(6*2)+(5*5)+(4*2)+(3*0)+(2*0)+(1*0)=95
95 % 10 = 5
So 162520-00-5 is a valid CAS Registry Number.
162520-00-5Relevant articles and documents
Hybrids from farnesylthiosalicylic acid and hydroxamic acid as dual ras-related signaling and histone deacetylase (HDAC) inhibitors: Design, synthesis and biological evaluation
Ling, Yong,Wang, Xuemin,Wang, Chenniu,Xu, Chenjun,Zhang, Wei,Zhang, Yihua,Zhang, Yanan
, p. 971 - 976 (2015)
Abstract A novel series of hybrids was designed and synthesized by combining key elements from farnesylthiosalicylic acid (FTS) and hydroxamic acid. Several 3,7,11-trimethyldodeca-2,6, 10-trien-1-yl) thio)benzamide derivatives, particularly those with bra
ANTI-INFLAMMATORY, ANTI-CANCER, AND ANTI-ANGIOGENIC COMPOUNDS, PHARMACEUTICALS COMPOSITIONS, AND METHODS OF MAKING AND USING THEREOF
-
, (2019/04/26)
Compounds of the general Formula A-D-Y are disclosed with activity towards treating diseases related to inflammation, cancer, neurodegenerative diseases, and cardiovascular diseases. Pharmaceutical compositions, methods of making, and methods of use there
Hybrid molecule from Farnesylthiosalicylic acid-diamine and phenylpropenoic acid as Ras-related signaling inhibitor with potent antitumor activities
Ling, Yong,Wang, Zhiqiang,Wang, Xuemin,Li, Xianghua,Wang, Xinyang,Zhang, Wei,Dai, Hong,Chen, Li,Zhang, Yihua
, p. 145 - 152 (2015/01/30)
Novel series of Farnesylthiosalicylic acid-diamine/phenylpropenoic acid hybrids were designed and synthesized. Their in vitro growth inhibitory assays showed that most compounds displayed strong antiproliferation activity against seven cancer cells. Especially, the new hybrid 12f, by the conjugation of 10a with ferulic acid, could selectively suppress the proliferation of tumor cells and display significantly lower toxicities to normal cells than its intermediate 10a. Furthermore, 12f dose-dependently induced SMMC-7721 cell apoptosis. Additionally, our observations demonstrated that 12f inhibited both Ras-related signaling and phosphorylated NF-κB synergistically, which may be advantageous to the strong antitumor activities of 12f. Our findings suggest that these novel hybrids may hold a great promise as therapeutic agents for the intervention of human cancers.