Sorafenib, p-Toluenesulfonate Salt (Sorafenib Tosylate, Nexavar, Bay 43-9006, DB00398, NSC-724772, CAS 475207-59-1), >99%

LC Laboratories' Product Number S-8502 - Sorafenib, p-Toluenesulfonate Salt (Sorafenib Tosylate, Nexavar, Bay 43-9006, DB00398, NSC-724772), >99% - for research use only. Sorafenib (Bay 43-9006) is a novel bi-aryl urea compound that inhibits cell proliferation by targeting the ERK pathway and angiogenesis by targeting the receptor tyrosine kinases VEGFR-2 and PDGFR-β and their associated signaling cascades. Although sorafenib was initially developed as a Raf kinase inhibitor (IC50 = 6 nM), it has since been shown to have activity against many receptor tyrosine kinases involved in tumorigenesis and angiogenesis including FGFR-1, wt BRAF and V599E mutant BRAF, as well as members of the so-called "split kinase" family: VEGFR-2, VEGFR-3, PDGFR-β, c-KIT, and Flt3. However, sorafenib is not active against erbB1, erbB2, ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-MET, c-yes, PKB, PKA, cdk1/cyclinB, PKC, and pim-1. In cellular mechanistic assays, sorafenib decreased basal phosphorylation of the ERK pathway in melanoma, breast, colon, and pancreatic tumor cell lines. Sorafenib is more potent in a cellular system (IC50 = 20 nM) than in an enzyme assay (IC50 = 107 nM). Sorafenib potently inhibited activation of the MAPK pathway and ERK phosphorylation in human cancer cell lines, irrespective of whether they harbored K-ras mutations, V599EB-Raf, or both. Sorafenib inhibited various nonkinase targets, including adenosine A3, dopamine D1, and muscarine M3 receptors, albeit at much higher (micromolar) concentrations than kinase targets. Sorafenib tosylate is the active ingredient in the drug sold under the trade name Nexavar®. This drug has been approved in at least one country for use in patients with advanced renal cell cancer.

• Supplier: LC Laboratories
• Product #: S-8502
• Sku #: S-8502_1g