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assay
>95% (TLC)
form
lyophilized powder
mol wt
~464.8
shipped in
ambient
storage temp.
−20°C
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.
signalword
Danger
hcodes
Hazard Classifications
Aquatic Acute 1 - Aquatic Chronic 1 - Lact. - Repr. 1B - STOT RE 1
Storage Class
6.1D - Non-combustible acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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