Sorafenib (BAY 43-9006) is biarylurea-based inhibitor of Raf1 (IC50, 6 nM) with additional activity against B-Raf, mVEGFR2, mPDGFRb (IC50, 22 nM, 15 nM, and 57 nM respectively), and related kinases. [1] In MDA-MB-231 breast cancer cells, sorafenib efficiently blocks activation of the MAPK pathway. Dose-dependent inhibition of basal MEK 1/2 and ERK 1/2 phosphorylation was observed at IC50s of 40 and 100 nM, respectively. [1]
In hepatocellular carcinoma cell lines, sorafenib inhibited cell proliferation in a dose-dependent manner with an IC50 of 6.3 uM in PLC/PRF/5 and 4.5 uM in HepG2 cells. [2] Flow cytometry studies indicated a decrease in G1 and increase of S phase after sorafenib treatment in HepG2 cells.
Technical information:
Chemical Formula: | C21H16ClF3N4O3 | |
CAS #: | 284461-73-0 | |
Molecular Weight: | 464.82 | |
Purity: | >99% | |
Appearance: | White | |
Chemical Name: | 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide | |
Solubility: | Up to 100mM in DMSO | |
Synonyms: | Sorafenib, Nexavar, sorafenibum, BAY-43-9006 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Wilhelm 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. 2004, 64, 7099-7109. Pubmed ID: 15466206 |
2. | Liu et al., Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Cancer Res. 2006, 66, 11851-11858. Pubmed ID: 17178882 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.