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PF-8380

Chemical Structure : PF-8380

CAS No.: 1144035-53-9

PF-8380 (PF 8380, PF8380)

Catalog No.: PC-43508Not For Human Use, Lab Use Only.

PF-8380 (PF8380) is a potent, specific, orally active Autotaxin inhibitor with IC50 of 2.8 and 101 nM in enzyme assay and in human whole blood assay, respectively.

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Biological Activity

PF-8380 (PF8380) is a potent, specific, orally active Autotaxin inhibitor with IC50 of 2.8 and 101 nM in enzyme assay and in human whole blood assay, respectively.
PF-8380 produces >95% reduction in both plasma and air pouch lysophosphatidic acid (LPA) within 3 h by dosed orally at 30 mg/kg in rat air pouch model.
PF-8380 reduces inflammatory hyperalgesia in vivo.
PF-8380 also enhances the radiosensitivity of human and murine glioblastoma cell lines.

Physicochemical Properties

M.Wt 478.33
Formula C22H21Cl2N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Piperazinecarboxylic acid, 4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-, (3,5-dichlorophenyl)methyl ester

References

1. Gierse J, et al. J Pharmacol Exp Ther. 2010 Jul;334(1):310-7.

2. Bhave SR, et al. Front Oncol. 2013 Sep 17;3:236.

3. St-Cœur PD, et al. Arch Pharm (Weinheim). 2013 Feb;346(2):91-7.

4. Navab M, et al. J Lipid Res. 2015 Apr;56(4):871-87.

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