PF-8380

SKU: orb1303978

Description

PF-8380 is a potent, orally bioavailable autotaxin inhibitor that effectively lowers lysophosphatidic acid (LPA) levels in vitro and in vivo. It is widely used in research on fibrosis, cancer, and inflammatory diseases, demonstrating efficacy in reducing LPA at inflammation sites in experimental models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1144035-53-9
• MW: 478.33
• Purity: 99.45% (May vary between batches)
• Formula: C₂₂H₂₁Cl₂N₃O₅
• SMILES: Clc1cc(Cl)cc(COC(=O)N2CCN(CCC(=O)c3ccc4[nH]c(=O)oc4c3)CC2)c1
• Target: PDE
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ATX:2.8 nM
• In Vivo:
  PF-8380 inhibits autotoxin in rat substrates (IC50: 1.16 nM) and demonstrates inhibition in human whole blood with an IC50 of 101 nM after 2 hours of treatment . Furthermore, PF-8380 suppresses autotoxin in GBM cells, subsequently reducing their invasion and migration capabilities while enhancing radiation sensitization.
• In Vitro:
  Pre-treatment with PF-8380 before radiotherapy can inhibit radiation-induced angiogenesis in tumor endothelial cells and delay the growth and development of intracranial glioma tumors. In a rat air pouch inflammation model, PF8380 (30 mg/kg, p.o.) reduced inflammatory pain sensitivity and decreased LPA levels in plasma and inflamed tissues by more than 95% within 3 hours.
• Cell Research:
  GL261 or U87-MG cells are plated in triplicate onto 6 cm plates and allowed to grow to 70% confluence. The semi-confluent cell layer is scratched with a sterile 200 μL pipette tip to create a scratch devoid of cells and plates are washed once with PBS to remove non-adherent cells and debris. For radiosensitization drug studies, cells are treated with 1 μM PF-8380 or DMSO for 45 min prior to irradiation with 4 Gy, and then incubated at 37°C in 5% CO2. Control plates are monitored for cell migration (20–24 h). Cells are fixed with 70% ethanol and stained with 1% methylene blue. To quantify migration, cells in three randomly selected high power fields (HPFs) in the scratched area are counted and normalized for surrounding cell density.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autotaxin, inhibit, Inhibitor, PF 8380, PF8380, PF-8380, phosphodiesterase, Phosphodiesterase (PDE)

Compound Identifiers

PubChem CID

25265312