PF-8380 CAS: 1144035-53-9
MF: C22H21Cl2N3O5
MW: 478.33
A substrate competitive and tight-binding inhibitor of autotaxin.

PF-8380 (CAS 1144035-53-9)

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Synonym: 6-(3-(piperazin-1-yl)propanoyl)benzo(d)oxazol-2(3H)-one
Application: A substrate competitive and tight-binding inhibitor of autotaxin
CAS Number: 1144035-53-9
Molecular Weight: 478.33
Molecular Formula: C22H21Cl2N3O5
* Refer to Certificate of Analysis for lot specific data (including water content).
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PF-8380 is an orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}.


References

PMID: 20392816

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), water (slightly), DMF (~5 mg/ml), and DMF:PBS (pH 7.2)(1:6) (~0.14 mg/ml).
Storage :
Store at -20° C
Melting Point :
117-123° C
Density :
1.42 g/cm3
Refractive Index :
n20D 1.62 (Predicted)
IC50 :
autotaxin: IC50 = 1.15 nM (Fetal fibroblast cell-LPC); autotaxin: IC50 = 1.16 nM (Rat/murine enzyme-FS-3); autotaxin : IC50 = 1.7 nM ( recombinant human enzyme-β isoform employing LPC (lysophosphatidylcholine) as substrates); Potent autotaxin inhibitor in isolated enzyme assay: IC50 = 2.8 nM; Potent autotaxin inhibitor in human whole blood: IC50 = 101 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
25265312
MDL Number :
MFCD20527274
SMILES :
C1CN(CCN1CCC(=O)C2=CC3=C(C=C2)NC(=O)O3)C(=O)OCC4=CC(=CC(=C4)Cl)Cl

Download SDS (MSDS)

Certificate of Analysis

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