| 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. Appearance: Supplied as an off-white powder. Purity: HPLC: 99% TLC: 99% Solubility: Soluble in DMSO at 200mg/ml, soluble in ethanol at 3.3mg/ml with warming, very poorly soluble in water, maximum solubility in plain water is estimated to be about 10-50uM, buffers, serum, or other additives may increase or decrease the aqueous solubility. Melting Point: 204-206.5C Elemental Anaylsis: Calculated: C=54.26% H=3.47% Cl=7.63% F=12.26% N=12.05% Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20C. For maximum recovery of product, centrifuge the original vial prior to removing the cap. |
