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Sorafenib | Inhibitor of Raf-1 and other kinases

Sorafenib (475207-59-1; base) was initially developed as a Raf kinase inhibitor, IC50 = 6 nM, but has been shown to inhibit many receptor tyrosine kinases including BRAF (IC50 = 22 nM); VEGFR-2 (IC50 = 90 nM); VEGFR-3 (IC50 = 20 nM); PDGFR-β (IC50 = 57 nM); Flt3 (IC50 = 58 nM); c-KIT (IC50 = 68 nM); FGFR-1 (IC50 = 580 nM).1 Paradoxically more potent in a cellular assay (IC50 = 20 nM) compared to an isolated enzyme assay (IC50 = 107 nM) for c-Fms.2 Inhibits activation of MAPK pathway and ERK phosphorylation.3 Induces caspase-independent apoptosis in melanoma cells.4 Sorafenib is a clinically useful anticancer agent.

References/Citations
1) Wilhelm et al. (2004), 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
2) Guo et al. (2006), 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
3) Wilhelm et al. (2003), The novel Raf inhibitor BAY 43-9006 blocks signaling and proliferation in BRAF mutant and wildtype melanoma and colorectal tumor cell lies; Proc. Am. Assoc. Cancer Res., 44 106609
4) Panka et al. (2006), The Raf inhibitor BAY 43-9006 (Sorafenib) induces caspase-independent apoptosis in melanoma cells; Cancer Res., 66 1611

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Catalog#  10-2174

$40.00
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CAS:
475207-59-1
Catalog Number:
10-2174
Activity:
Inhibitor of Raf-1 and other kinases
Alternate Names:
BAY 43-9006
Chemical Name:
4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide
Molecular Weight:
464.83
Molecular Formula:
C21H16ClF3N4O3
Solubility:
Soluble in DMSO (up to 200 mg/ml) or in Ethanol (up to 3 mg/ml).
Physical Properties:
Off-white solid
Purity:
99% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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