PF 8380

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Cat.No. 4078 - PF 8380 | C22H21Cl2N3O5 | CAS No. 1144035-53-9
Description: Potent autotaxin inhibitor
Chemical Name: 3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent autotaxin inhibitor (IC50 = 2.8 nM in isolated enzyme assay; 101 nM in human whole blood). Modulates lysophosphatidic acid (LPA) levels in vivo and in vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at site of inflammation. Orally available.

Technical Data

M. Wt 478.33
Formula C22H21Cl2N3O5
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1144035-53-9
PubChem ID 25265312
InChI Key JMSUDQYHPSNBSN-UHFFFAOYSA-N
Smiles O=C(C2=CC(OC(N4)=O)=C4C=C2)CCN1CCN(C(OCC3=CC(Cl)=CC(Cl)=C3)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.83 100

Preparing Stock Solutions

The following data is based on the product molecular weight 478.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.09 mL 10.45 mL 20.91 mL
5 mM 0.42 mL 2.09 mL 4.18 mL
10 mM 0.21 mL 1.05 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Gierse et al (2010) A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J.Pharmacol.Exp.Ther. 334 310 PMID: 20392816

Jankowski (2011) Autotaxin: its role in biology of melanoma cells and as a pharmacological target. Enzyme Res. 194857 PMID: 21423677


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Cancer

Cancer Research Product Guide

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