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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
Certificates of Analysis (COA)
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Bei Zhou et al.
Molecular therapy. Nucleic acids, 26, 1051-1065 (2021-11-18)
Emerging evidence has shown that endoplasmic reticulum (ER) stress promotes sorafenib resistance in hepatocellular carcinoma (HCC). However, the underlying mechanisms are poorly understood. The purpose of this study was to explore the mechanism by which ER stress promotes sorafenib resistance
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