纯度:99% by HPLC;NMR (Conforms)
分子式:C15H8ClF5N2O3
分子量:394.68
溶剂:DMSO (>25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):Sorafenib analog with unique antibacterial properties
Function / Pharmacology:PK150 is a Sorafenib analog that displays significant antibacterial activity against several pathogenic strains (S.aureus NCTC8325, MIC = 0.3 μM; vancomycin -resistant enterococci, MIC = 3 μM; and M.tuberculosis MIC = 2 μM). It was inactive against Gram-negative bacteria. It effectively reduced persister cells in ciprofloxacin-treated stationary S.aureus cultures and effectively eradicated staphylococcus biofilms. PK150 did not develop antibacterial resistance in an agar-plate-based assay. Its antibacterial properties were attributed to demethylmenaquinone methyltransferase (MenG) inhibition and signal peptidase IB (SpsB) activation. PK150 displayed in vivo efficacy in a murine bloodstream infection model against methicillin-sensitive S. aureus and a neutropenic mouse thigh model against methicillin-resistant S. aureus strain ATCC33591. Inactive against a panel of over 250 human kinases.