纯度:99% by TLC,;NMR (Conforms)
分子式:C21H16ClF3N4O3
分子量:464.83
溶剂:DMSO (200 mg/ml) Ethanol (3 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):Raf-1 inhibitor (and other kinases)
Function / Pharmacology: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.