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AZ PFKFB3 26

Cat. No. M6479
AZ PFKFB3 26 Structure
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Biological Activity

AZ PFKFB3 26 is a potent and selective PFKFB3 inhibitor (IC50 = 0.023 μM). Selective for PFKFB3 over PFKFB2 and PFKFB1 isoforms (IC50 values are 0.382 μM and 2.06 μM, respectively). Reduces levels of fructose-1,6-bisphosphate in A549 cells (IC50 = 0.343 μM). Exhibits no significant inhibition of other kinases.

Chemical Information
Molecular Weight 402.49
Formula C24H26N4O2
CAS Number 1704740-52-2
Solubility (25°C) DMSO 40.25 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] Carroll, et al. Mol Pharmacol. BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.

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AZ-PFKFB3-67 quarterhydrate 

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AZ-PFKFB3-67 

AZ-PFKFB3-67 is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively.

PFK-158

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.

3PO

3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines with IC50 of 1.4-24 μM.

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