3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Chemical Properties

Melting point:

190-195 °C

Boiling point:

533.2±50.0 °C(Predicted)

Density 

1.464±0.06 g/cm3(Predicted)

storage temp. 

Inert atmosphere,Room Temperature

solubility 

Soluble in DMSO (up to at least 25 mg/ml)

form 

solid

pka

9.13±0.50(Predicted)

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Usage And Synthesis

Description

PF-06840003 (198474-05-4) is a potent (IC50?= 150 and 410 nM via two methods) and selective inhibitor of Indoleamine-2,3-dioxygenase (IDO1).1?In mice with syngeneic tumor grafts, it reduced intratumoral kynurenine levels by over 80%, inhibited tumor growth as monotherapy, and increased the efficacy of anti-PD-L1 therapy.2?PF-06840003 treatment combined with GM-CSF-secreting allogenic pancreatic tumor cell vaccine (GVAX) resulted in increased antitumor efficacy in a murine model of pancreatic ductal adenocarcinoma.3

Uses

PF-06840003 is a potential clinical candidate as a novel and selective Indoleamine 2,3-dioxygenase inhibitor. Highly selective and orally bioavailable IDO-1 inhibitor.

References

1) Crosignani?et al.?(2017),?Discovery of a Novel and Selective Indoleamine-2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EROS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate;?J. Med. Chem.?60?9617 2) Gomes?et al.?(2018),?Characterization of the Selective Indoleamine-2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy;?Mol. Cancer Ther.?9?2530 3) Blair?et al.?(2019),?IDO1 inhibition potentiates vaccine-induced immunity against pancreatic adenocarcinoma;?J. Clin. Invest.?129?1742

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