| Identification | Back Directory | [Name]
3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione | [CAS]
198474-05-4 | [Synonyms]
EOS200271
PF-06840003
PF-06840003 (racemate)
PF 06840003;PF-06840003
3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione
3-(5-Fluoro-1H-indol-3-yl)-2,5-pyrrolidinedione
2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)- | [Molecular Formula]
C12H9FN2O2 | [MDL Number]
MFCD25121820 | [MOL File]
198474-05-4.mol | [Molecular Weight]
232.21 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Room Temperature | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml) | [form ]
solid | [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. |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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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