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PK150

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Chemical Structure| 2165324-62-7 同义名 : -
CAS号 : 2165324-62-7
货号 : A1219208
分子式 : C15H8ClF5N2O3
纯度 : 99%+
分子量 : 394.681
MDL号 : MFCD32667017
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(633.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Methicillin-resistant Staphylococcus aureus (MRSA) is a cause of severe staph infections. PK150 is an analogue of sorafenib that shows 10-fold enhanced anti-MRSA activity. The minimal inhibitory concentration (MIC) of PK150 against MRSA was 0.3-1µM. PK150 also inhibited the methicillin-sensitive strain NCTC 8325 with a MIC of 0.3µM. PK150 at 1.2 and 2.4μM disintegrated S. aureus cells as evidenced by enhanced membrane permeability. The treatment of S. aureus ATCC 29213 bacteria cells with PK150 (2.4μM) for 196h fully eradicated persister cells. The incubation with PK150 at various doses (5, 25, and 50μM) for 80 min inhibited menaquinone-2 synthesis in MenG-overexpressing cells. In a neutropenic mouse thigh model, repeated dosing of PK150 (20mg/kg, p.o.) at 30min, 4h, and 8h after the inoculation of MRSA strain ATCC 33591 resulted in a 10-fold reduction in CFU/g in thighs compared to the vehicle-treated group[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.67mL

2.53mL

1.27mL

25.34mL

5.07mL

2.53mL
参考文献

[1]Le P, Kunold E, Macsics R, et al. Repurposing human kinase inhibitors to create an antibiotic active against drug-resistant Staphylococcus aureus, persisters and biofilms. Nat Chem. 2020;12(2):145-158. doi:10.1038/s41557-019-0378-7