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| | 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Basic information |
| Product Name: | 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione | | Synonyms: | 2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)-;3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione;3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione;PF-06840003;PF 06840003;PF-06840003;EOS200271;PF-06840003 (racemate);3-(5-Fluoro-1H-indol-3-yl)-2,5-pyrrolidinedione | | CAS: | 198474-05-4 | | MF: | C12H9FN2O2 | | MW: | 232.21 | | EINECS: | | | Product Categories: | API | | Mol File: | 198474-05-4.mol |  |
| | 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 |
| | 3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Preparation Products And Raw materials |
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