PF-8380

PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

Product Specifications

CAS Number

[1144035-53-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/PF-8380.html

Purity

99.05

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1CCN(CC1)CCC(C2=CC(O3)=C(C=C2)NC3=O)=O)OCC4=CC(Cl)=CC(Cl)=C4

Molecular Formula

C22H21Cl2N3O5

Molecular Weight

478.33

Precautions

H302, H315, H319, H335

References & Citations

[1]Gierse J, et al. A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J Pharmacol Exp Ther. 2010 Jul;334 (1) :310-7.|[2]Bhave SR, et al. Autotaxin Inhibition with PF-8380 Enhances the Radiosensitivity of Human and Murine Glioblastoma Cell Lines. Front Oncol. 2013 Sep 17;3:236.|[3]Cao P, et al. Autocrine lysophosphatidic acid signaling activates β-catenin and promotes lung allograft fibrosis. J Clin Invest. 2017 Apr 3;127 (4) :1517-1530.