Sorafenib (base)

• Background:

  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-Fms2. Inhibits activation of MAPK pathway and ERK phosphorylation3. Induces caspase-independent apoptosis in melanoma cells4. Clinically useful anticancer agent.

• Conjugation:

  Unconjugated

• Buffer:

  Off-white solid

• Storage Conditions:

  -20°C