[CAS NO. 1144035-53-9] PF-8380
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PRODUCTS SPECIFICATIONS [1144035-53-9]
Store
Catalog
SLK-S8218
Brand
Selleck
CAS
1144035-53-9
DESCRIPTION [1144035-53-9]
Overview
| MDL | MFCD20527274 |
|---|---|
| Molecular Weight | 478.33 |
| Molecular Formula | C22H21Cl2N3O5 |
| SMILES | O=C(N1CCN(CCC(C2=CC=C3NC(OC3=C2)=O)=O)CC1)OCC4=CC(Cl)=CC(Cl)=C4 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
PF-8380 is a potent inhibitor with of 2.8 nM in an in vitro enzyme assay.
Targets
| Autotaxin [1] (Cell-free assay) |
| 2.8 nM |
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.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.
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. 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.
References
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