Merck, 553018-5MG, RAF Kinase Inhibitor VII

General description
A cell-permeable imidazopyridinyl-urea compound that acts as a potent inhibitor against B-RafV⁶⁰⁰E activity (IC₅₀ = 1 nM) by targeting its ATP-binding pocket and the adjacent lipophilic allosteric site accessible only when the enzyme is in its inactive DFG-out conformation. Reported to effectively inhibit RafV⁶⁰⁰E-dependent ERK phosphorylation (IC₅₀ = 610 nM) and growth of human melanoma WM266.4 cells (GI₅₀ = 470 nM).
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Menard, D., et al. 2009. J. Med. Chem.52, 3881.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)