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Raf Kinase Inhibitor V
Propane-1-sulfonic acid-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl)-amide, PLX4720
A cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound's preferential binding and inhibitory activity toward the active Raf mutants (IC50 = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1Y340D/Y341D, B-RafV600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-RafV600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily, p.o.).
产品信息
Form Orange-yellow solid
Molar mass 413.8
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO or EtOH
Chemical formula C17H14ClF2N3O3S
CAS number 918505-84-7
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |