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PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $85 | In Stock | In Stock | |
| 25 mg | $109 | In Stock | In Stock | |
| 50 mg | $129 | In Stock | In Stock | |
| 100 mg | $198 | - | In Stock | |
| 200 mg | $297 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock | In Stock |
| Description | PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor. |
| Targets&IC50 | IDO1 (human):0.41 μM, IDO1 (mouse):1.5 μM, dIDO1:0.59 μM |
| In vitro | The s of PF-06840003 has inhibitory for hIDO-1 (IC50: 0.41 μM), mouse IDO-1 (IC50: 1.5 μM) and dog IDO-1 (IC50: 0.59 μM), respectively. It has very weak inhibitory against hTDO-2 (IC50: 140 μM). In cellular assays, PF-06840003 shows activity both in the LPS/INFγ-stimulated THP1 cells (IC50: 1.7 μM) and in the HeLa assay (IC50: 1.8 μM). PF-06840003 is a very weak inhibitory against CYPs (IC50>100 μM) except 2C19 (IC50: 78 μM). |
| In vivo | In mice, PF-06840003 reduces intratumoral kynurenine levels (>80%). In multiple preClinicalal syngeneic models in mice, It inhibits tumor growth by combinated with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours. |
| Synonyms | PF 06840003, EOS200271 |
| Molecular Weight | 232.21 |
| Formula | C12H9FN2O2 |
| Cas No. | 198474-05-4 |
| Smiles | Fc1ccc2[nH]cc(C3CC(=O)NC3=O)c2c1 |
| Relative Density. | 1.464 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (258.39 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.61 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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