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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF-8380 is a specific and potent inhibitor of Autotaxin (ATX) with an IC50 value of 2.8 nM [1].
Autotaxin (ATX) is a secreted enzyme having lysophospholipase D activity
Cell lines
Mouse glioma GL261 cell lines, Human glioblastoma (U87-MG) cells
Preparation method
Soluble in DMSO > 20.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
1 μM, 45min
Applications
Pre-treatment of GL261 and U87-MG cells with 1mM PF-8380 followed by 4 Gy irradiation resulted in decreased clonogenic survival, decreased migration, decreased invasion, and attenuated radiation-inducedAkt(protein kinase B) phosphorylation.
Animal models
Female Lewis rats
Dosage form
10, 30, 100 mg/kg, b.i.d, oral administration
Application
The specific inhibitor PF-8380 provided >95% reduction in both plasma and air pouch LPA (lysophosphatidic acid), indicating autotaxin is a major source of LPA during inflammation. PF-8380 reduced inflammatory hyperalgesia with the similiar efficacy as naproxen.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Bhave SR1, Dadey D, et al, Autotaxin Inhibition with PF-8380 Enhances the Radiosensitivity of Human and Murine Glioblastoma Cell Lines. Front Oncol. 2013 Sep 17;3:236. doi: 10.3389/fonc.2013.00236. eCollection 2013.
[2]. Gierse J1, Thorarensen A, 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. doi: 10.1124/jpet.110.165845. Epub 2010 Apr 14.