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PFK-158

Cat. No. M6727
PFK-158 Structure
Synonym:

ACT-PFK-158

Size Price Availability Quantity
10mM*1mL in DMSO USD 85  USD85 In stock
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 220  USD220 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

PFK-158, also known as ACT-PFK-158, is a potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) with potential antineoplastic activity.

Chemical Information
Molecular Weight 328.29
Formula C18H11F3N2O
CAS Number 1462249-75-7
Solubility (25°C) DMSO: ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Liqiong Chen, et al. Synergistic Activity and Biofilm Formation Effect of Colistin Combined with PFK-158 Against Colistin-Resistant Gram-Negative Bacteria

[2] Upasana Ray, et al. Group III phospholipase A2 downregulation attenuated survival and metastasis in ovarian cancer and promotes chemo-sensitization

[3] Wei Wang, et al. Design, synthesis, and antibacterial evaluation of PFK-158 derivatives as potent agents against drug-resistant bacteria

[4] Krzysztof Kotowski, et al. Role of PFKFB3 and PFKFB4 in Cancer: Genetic Basis, Impact on Disease Development/Progression, and Potential as Therapeutic Targets

[5] Youwen Zhang, et al. Synergistic Effect of Colistin Combined with PFK-158 against Colistin-Resistant Enterobacteriaceae

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  Catalog
Abmole Inhibitor Catalog




Keywords: PFK-158, ACT-PFK-158 supplier, PFKFB3, inhibitors, activators


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