ChemicalBook CAS DataBase List 2165324-62-7

2165324-62-7

Name	PK150
CAS	2165324-62-7
Molecular Formula	C15H8ClF5N2O3
MDL Number	MFCD32667017
Molecular Weight	394.68
MOL File	2165324-62-7.mol

Chemical Properties

Boiling point	322.1±42.0 °C(Predicted)
density	1.63±0.1 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (up to at least 25 mg/ml).
form	solid
pka	12.44±0.40(Predicted)
color	White
Stability:	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P280-P301+P312-P302+P352-P305+P351+P338

Hazard Information

Description

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.

Uses

PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively[1].

in vivo

The in vivo efficacy of PK150 against methicillin-sensitive S. aureus (MSSA) (strain SH1000) is demonstrated in a murine bloodstream infection model. PK150 (20?mg/kg; p.o.) significantly reduces bacterial loads in the liver and heart^[1].
PK150 (10 and 20mg/kg orally; or 10mg/kg intravenously) shows no obvious signs of toxicity in mice. Higher i.v. dosing of 20mg/kg results in severe toxic effects and is thus avoided for subsequent therapeutic models^[1].

Animal Model:	Pathogen-free 9-week old female C57BL/6J mice^[1]
Dosage:	20?mg/kg
Administration:	Administered p.o.
Result:	Bacterial loads in the liver and heart were both significantly reduced by approximately 100-fold.

Animal Model:	Outbred male CD-1 mice, 4 weeks old^[1]
Dosage:	10 and 20 mg/kg (Pharmacokinetic Analysis)
Administration:	Administered by intragastric gavage at 10 and 20 mg/kg or intravenously at 10 mg/kg
Result:	Oral bioavailability was approximately 63% and the mean residence time was slightly enhanced via this administration route. T_1/2=11.69±1.5, 9.67±0.2, and 9.37±0.5 hours for 10 mg/kg i.v., 10 mg/kg p.o., and 20 mg/kg p.o., respectively.

References

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

Spectrum Detail

Supplier

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