PFI 653

Product Description

PFI 653 is a potent and selective vanin 1 inhibitor (IC₅₀ values in the range 6.85 - 24.5 nM). The compound exhibits selectivity over a panel of 40 kinases and a selection of 35 other targets including enzymes, receptors and ion channels (IC₅₀ vs biotinidase > 50 μM). Following administration of a single dose of PFI 653 (2 mg/kg iv) in rats AUC is 1790 ng.h/mL, half-life is 1 h and clearance is 19 mL/min/kg. Following oral administration of PFI 653 in solution, bioavailablility is 96%. In mice with DSS-induced inflammatory bowel disease (IBD), oral adminstration of PFI 653 dose-dependently reduces vanin 1 enzyme activity and disease symptoms.

Licensing Information

This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI-653 probe summary on the SGC website.

Solubility

Preparing Stock Solutions for PFI 653

The following data is based on the product molecular weight 354.41

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.82 mL	14.11 mL	28.22 mL
5 mM	0.56 mL	2.82 mL	5.64 mL
10 mM	0.28 mL	1.41 mL	2.82 mL
50 mM	0.06 mL	0.28 mL	0.56 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Casimiro-Garcia Discovery of a series of pyrimidine carboxamides as inhibitors of vanin-1. J.Med.Chem. 2022 PMID: 34967602