An inhibitor of IDO-1
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EOS200271

Item No. 25003

Technical Information
Formal Name
3-(5-fluoro-1H-indol-3-yl)-2,5-pyrrolidinedione
CAS Number
198474-05-4
Synonyms
  • PF-06840003
Molecular Formula
C12H9FN2O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
221, 287 nm
SMILES
FC1=CC=C2C(C(C3CC(NC3=O)=O)=CN2)=C1
InChi Code
InChI=1S/C12H9FN2O2/c13-6-1-2-10-7(3-6)9(5-14-10)8-4-11(16)15-12(8)17/h1-3,5,8,14H,4H2,(H,15,16,17)
InChi Key
MXKLDYKORJEOPR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    EOS200271 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1; IC50 = 0.15 µM for the human enzyme).1 It is selective for IDO-1 over IDO-2 up to a concentration of 200 µM for the human recombinant enzymes. EOS200271 inhibits IDO-1-mediated production of kynurenine induced by IFN-γ in HeLa cells (IC50 = 1.8 µM) and by LPS and IFN-γ in THP-1 cells and human-derived whole blood ex vivo (IC50s = 1.7 and 4.7 µM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Crosignani, S., Bingham, P.M., Bottemanne, P., et alDiscovery of a novel and selective indoleamine 2,3-dioxygenase (IDO-1) inhibitor 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and its characterization as a potential clinical candidate. J. Med. Chem. 60(23), 9617-9629 (2017).