PFI 653

Name: PFI 653
Brand: Tocris Bioscience
SKU: 7963

Tocris Bioscience, part of Bio-Techne | Catalog # 7963

COA / SDS

Potent and selective vanin 1 inhibitor

Key Product Details

Description:	Potent and selective vanin 1 inhibitor
Chemical Name:	8-Oxa-2-azaspiro[4.5]dec-2-yl[2-[(2-pyrazinylmethyl)amino]-5-pyrimidinyl]methanone
Purity:	≥98% (HPLC)
Molecular Weight:	354.41

View Full Technical Details for PFI 653

Technical Data
Citations

Biological Activity for PFI 653

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.

Technical Data for PFI 653

M. Wt	354.41
Formula	C₁₈H₂₂N₆O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2173134-00-2
PubChem ID	134177597
InChi Key	VGRLXWFIXGZRMS-UHFFFAOYSA-N
Smiles	O=C(C1=CN=C(N=C1)NCC2=NC=CN=C2)N3CCC4(C3)CCOCC4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PFI 653

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	1.77	5
	DMSO	35.44	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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Reconstitution Calculator

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References for PFI 653

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