PF-06840003 (racemate)
EOS200271；3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione
CAS: 198474-05-4
Molecular Formula: C12H9FN2O2
PF-06840003 (racemate) - Names and Identifiers
PF-06840003 (racemate) - Physico-chemical Properties
| Molecular Formula | C12H9FN2O2 |
| Molar Mass | 232.21 |
| Solubility | DMSO : 28 mg/mL (120.58 mM) |
| Appearance | solid |
| Color | White |
| Storage Condition | Inert atmosphere,Room Temperature |
| 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. |
| In vitro study | PF-06840003 is a racemic mixture. Its IC50 for human IDO-1, murine IDO-1, and canine IDO-1 were 0.41, 1.5, and 0.59 μm, respectively. PF-06840003 has only very weak activity against hTDO-2, with an IC50 of 140 μm. In cell experiments, PF-06840003 was active in both Hela cells and LPS/infγ-stimulated THP1 cells with IC50 of 1.8 μm and 1.7 μm, respectively. The inhibitory effect of PF-06840003 on CYPs is very weak, and the IC50 of most CYP isoenzymes is greater than 100 μm (except for 2C19,IC50=78 μm). In addition, PF-06840003 had no metabolism-dependent inhibition of the CYP enzymes involved in the assay. |
| In vivo study | PF-06840003 in vivo half-life is about 16-19 hours. Its oral bioavailability in mice, rats and dogs was 59%,94% and 19%, respectively. PF-06840003 monotherapy has significant antitumor activity in Pan02, B16 − F10, CT26, MC38, 4T1, and renal cell carcinoma models; In the CT26 model, PF-06840003 and anti-PDL1 mAb have a synergistic effect. PF-06840003 has a good pharmacokinetic profile in vivo with low/moderate clearance in most preclinical animals. In rats, PF-06840003 can penetrate the central nervous system, indicating its potential in brain metastases. |
PF-06840003 (racemate) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.306 ml | 21.532 ml | 43.064 ml |
| 5 mM | 0.861 ml | 4.306 ml | 8.613 ml |
| 10 mM | 0.431 ml | 2.153 ml | 4.306 ml |
| 5 mM | 0.086 ml | 0.431 ml | 0.861 ml |
Last Update：2024-01-02 23:10:35
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Product Name: EOS200271；3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Visit Supplier Webpage Request for quotationCAS: 198474-05-4
Tel: 18301782025
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Spot supply
Product Name: EOS200271；3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione Visit Supplier Webpage Request for quotationCAS: 198474-05-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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