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5MPN

Cat. No. M45095
5MPN Structure
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Biological Activity

5MPN is a first-in-class, orally active and selective inhibitor of fructose-6-phosphate-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), which does not inhibit PFK-1 or PFKFB3. 5MPN is a competitive inhibitor of the F6P-binding site (Ki=8.6 μM). 5MPN inhibits proliferation of various cancer cell lines by targeting tumor glucose metabolism. 5MPN is a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN can inhibit the proliferation of various cancer cell lines by targeting tumor glycolysis.

Chemical Information
Molecular Weight 305.33
Formula C15H19N3O4
CAS Number 47208-82-2
Form Solid
Solubility (25°C) DMSO 100 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.

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