PF-8380

• Description :

  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.

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  Autotaxin

• CAS Number :

  [1144035-53-9]