SORAFENIB

Application

Clinically useful anticancer agent.

Biochem/physiol Actions

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-beta (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⁾.

Reconstitution

Formulated as a lyophilized powder. May be dissolved in DMSO (200 mg/mL) or Ethanol (3 mg/mL).

Storage and Stability

Store desiccated as supplied at -20°C for up to 2 years. Store solutions at -20°C for up to 1 month.