3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
- CAS NO.:198474-05-4
- Empirical Formula: C12H9FN2O2
- Molecular Weight: 232.21
- MDL number: MFCD25121820
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione?
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
The Uses of 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
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
Properties of 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
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. |
Safety information for 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
Computed Descriptors for 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
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