Sorafenib, p-Toluenesulfonate Salt (4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide Tosylate, Sorafenib Tosylate, Bay 43-9006, Nexavar, DB00398, NSC-724772)

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-b and their associated signaling cascades. Although sorafenib was initially developed as a Raf kinase inhibitor (IC50=6nM), 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-b, 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.\n\nSolubility:\nSoluble in DMSO at 200mg/ml; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

S5343-15

Size

1g

Form

Supplied as an off-white crystalline powder

Purity

~99%

References

1. Guo, J., et al. \"Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors.\" Mol. Cancer Ther. 5:1007-1013 (2006). 2. Wilhelm, S., et al. \"The novel Raf inhibitor Bay 43-9006 blocks signaling and proliferation in BRAF mutant and wildtype melanoma and colorectal tumor cell lines.\" Proc. Am. Assoc. Cancer Res. 44:106609 (2003). 3. Wilhelm, S.M., et al. \"BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis.\" Cancer Res. 64:7099-7109 (2004).