PK150 | Sorafenib analog with unique antibacterial properties

PK150 (2165324-62-7) 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.

References/Citations
1) Le et al. (2019) Repurposing human kinase inhibitors to create an antibiotic active against drug-resistant Staphylococcus aureus, persisters and biofilms; Nat. Chem. 12 145

Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

10 mg, 50 mg

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CAS:
2165324-62-7
Catalog Number:
10-3960
Activity:
Sorafenib analog with unique antibacterial properties
Chemical Name:
1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)urea
Molecular Weight:
394.68
Molecular Formula:
C15H8ClF5N2O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

PK150 | Sorafenib analog with unique antibacterial properties

$55.00$195.00

CAS:
2165324-62-7
Catalog Number:
10-3960
Activity:
Sorafenib analog with unique antibacterial properties
Chemical Name:
1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)urea
Molecular Weight:
394.68
Molecular Formula:
C15H8ClF5N2O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
  • 10 mg
  • 50 mg
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