PF-8380
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
- 1. Yaya Wang, Jie Zhang, et al. "The LPA-CDK5-Tau Pathway Mediates Neuronal Injury in an In Vitro Model of Ischemia-Reperfusion Insult." BMC Neurol. 2022 May 2;22(1):166. PMID:35501719
- 2. Wang C, Zhang J, et al. "Lysophosphatidic acid induces neuronal cell death via activation of asparagine endopeptidase in cerebral ischemia-reperfusion injury." Exp Neurol. 2018 Aug;306:1-9. PMID:29673933
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 478.33 |
| Cas No. | 1144035-53-9 |
| Formula | C22H21Cl2N3O5 |
| Synonyms | PF 8380;PF8380 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥20.9 mg/mL in DMSO |
| Chemical Name | 3,5-dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)propyl)piperazine-1-carboxylate |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC(COC(N2CCN(CCC(C(C=C3)=CC(O4)=C3NC4=O)=O)CC2)=O)=CC(Cl)=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Mouse glioma GL261 cell lines, Human glioblastoma (U87-MG) cells |
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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. |
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Reacting condition |
1 μM, 45min |
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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 experiment [2]: | |
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Animal models |
Female Lewis rats |
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Dosage form |
10, 30, 100 mg/kg, b.i.d, oral administration |
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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. |
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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. |
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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. |
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| Description | PF-8380 is a potent and specific inhibitor of autotaxin with an IC50 value of 2.8 nM in isolated enzyme assay. | |||||
| Targets | autotaxin | |||||
| IC50 | 2.8 nM | |||||
Quality Control & MSDS
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