Home Metabolism PDE inhibitor PF-8380 For research use only.

PF-8380

PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.

PF-8380 Chemical Structure

PF-8380 Chemical Structure

CAS No. 1144035-53-9

Purity & Quality Control

PF-8380 Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

Biological Activity

Description PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.
Targets
Autotaxin [1]
(Cell-free assay)
2.8 nM
In vitro
In vitro PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM with FS-3 substrate. In human whole blood incubated with compound for 2 h autotaxin was inhibited with an IC50 of 101 nM[1].Inhibition of autotaxin by PF-8380 leads to decreased invasion, migtation and enhanced radiosensitization of GBM cells. Radiation-induced activation of Akt is abrogated by inhibition of ATX. Furthermore, inhibition of ATX leads to diminished tumor vascularity and delayed tumor growth[2].
Cell Research Cell lines Mouse GL261 and Human U87-MG cells
Concentrations 1 μM
Incubation Time 45 min
Method 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.
In Vivo
In vivo Pre-treatment with PF-8380 prior to irradiation inhibited radiation-induced angiogenesis of tumor vascular endothelial cells and delayed progression of glioma tumor growth in vivo[2]. Oral administration of 30 mg/kg PF8380 reduces inflammatory hyperalgesia in a rat air pouch model, exhibiting >95% reduction of LPA levels in both plasma and inflammatory site tissue within 3 hours[1].
Animal Research Animal Models Male Lewis rats
Dosages 1, 3, 10, 30, and 100 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 478.33 Formula

C22H21Cl2N3O5
CAS No. 1144035-53-9 SDF Download PF-8380 SDF
Smiles C1CN(CCN1CCC(=O)C2=CC3=C(C=C2)NC(=O)O3)C(=O)OCC4=CC(=CC(=C4)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 2 mg/mL ( (4.18 mM) Ultrasonicated; Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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