Salirasib
162520-00-5
0.98%
2026-07-16
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName Salirasib Cat No CEI-1515 Description Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki value of 2.6 µM. Product Overview Salirasib (S-trans,trans-farnesylthiosalycilic acid [FTS]) is a synthetic small molecule that acts as a potent Ras inhibitor. The Ras family of small GTPases transmits extracellular signals, which are initiated by cell-surface receptors and serve to regulate various cellular processes including cell growth, differentiation, motility and cell death. Signals transmitted by activated Ras induce activation of multiple effectors. Ras signaling is activated in a large number of human cancers. Mutations of codons 12, 13 and 61 in Ras result in constitutively active Ras, and activating mutations of the three major Ras isoforms (H, K and N) have been found in more than 33% of human cancers. Salirasib mimics the carboxy-terminal farnesylcysteine carboxymethyl ester common to all Ras proteins, which acts as part of a recognition unit for anchorage and dislodges the active Ras protein from the cell membrane. Salirasib is readily taken up by cells, and once inside the cell it specifically disrupts the association of active forms of all Ras proteins (H-ras, K-ras and N-ras) with the inner surface of the cell membrane and with other cellular membranes. The in vitro activity of salirasib has been demonstrated in pancreatic cell lines and xenograft models. In the Panc-1 cell line, salirasib decreased the amount of RAS in a dosedependent manner, with a maximum decrease in Ras of approximately 50 % seen at concentrations of 25 to 50 μM. In the mouse xenograft models, salirasib inhibites Panc-1 tumor growth and is shown to be synergistic with gemcitabine, both inhibiting tumor growth and prolonging survival. Salirasib is tested in a phase I study in patients with solid tumors twice daily for 21 days every 4 weeks. Doses are escalated from 100 to 200, 400, 600, and 800 mg. Dose-limiting toxicity is not reached, but all three patients treated with 800 mg experienced Grade 1-2 diarrhea, preventing further dose escalation. The recommended dose for phase II studies is 600 mg bid. CAS No 162520-00-5 Molecular Weight 358.54 Purity 0.98 Storage Store at -20°C Synonyms S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS Targets PPMTase IC50 2.6 µM Molecular Formula C22H30O2S Chemical Name 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid Solubility Soluble in DMSO > 10 mM Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Inhibitors(c1514) cas_num 162520-00-5 Basic Info-
Product Name:
Farnesylthiosalicylic acid
Other Name: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;748188-28-5
CAS No.:162520-00-5
Molecular Formula:C22H30O2S
InChIKeys:InChIKey=WUILNKCFCLNXOK-CFBAGHHKSA-N
Molecular Weight:358.54
Exact Mass:358.54
UNII:MZH0OM550M
NSC Number:685986
NCI Thesaurus Code:C71146
Categories:
Characteristics-
PSA:
62.6
XLogP3:7.2
Appearance:white to beige
Density:1.05
Melting Point:64-66°C
Boiling Point:486.0±45.0 °C(Predicted)
Flash Point:247.7±28.7 °C
Refractive Index:1.559
Water Solubility:DMSO: soluble20mg/mL, clear
Storage Conditions:-20°C Freezer
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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