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Submit ReviewPFI 653
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)
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 Data 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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Product Datasheets for PFI 653
References for PFI 653
References are publications that support the biological activity of the product.
Casimiro-Garcia et al (2022) Discovery of a series of pyrimidine carboxamides as inhibitors of vanin-1. J.Med.Chem. 65 757 PMID: 34967602
If you know of a relevant reference for PFI 653, please let us know.
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