PF-06840003
Based on 1 publication(s) in Google Scholar
PF-06840003 (EOS200271) is a highly selective, orally active and brain-penetrant IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 198474-05-4
- Formula: C12H9FN2O2
- Molecular Weight:232.21
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-06840003
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Biological Activity
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IDO-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.21 μM
Compound: PF-06840003
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Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs
Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs
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[PMID: 30469041] |
| HeLa | IC50 |
1.8 μM
Compound: 6; EOS200271; PF-06840003
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Inhibition of IDO-1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine production after 16 to 24 hrs by PDMAB method
Inhibition of IDO-1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine production after 16 to 24 hrs by PDMAB method
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[PMID: 29111717] |
PF-06840003 reverses IDO-1-induced T-cell anergy in vitro[1]. PF-06840003 shows activity both in the HeLa assay (IC50=1.8 μM) as well as in the LPS/ INFγ-stimulated THP1 cells (IC50=1.7 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 198474-05-4
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Appearance Solid
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Molecular Weight 232.21
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Formula C12H9FN2O2
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Color Light yellow to yellow
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SMILES
O=C(C(C1=CNC2=C1C=C(F)C=C2)C3)NC3=O
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Synonyms
EOS200271
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
2023 Aug 17;30(8):987-998.e24. PMID: 37490918
Solvent & Solubility
DMSO : ≥ 100 mg/mL (430.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3064 mL | 21.5319 mL | 43.0637 mL | 107.6593 mL |
| 5 mM | 0.8613 mL | 4.3064 mL | 8.6127 mL | 21.5319 mL | |
| 10 mM | 0.4306 mL | 2.1532 mL | 4.3064 mL | 10.7659 mL | |
| 15 mM | 0.2871 mL | 1.4355 mL | 2.8709 mL | 7.1773 mL | |
| 20 mM | 0.2153 mL | 1.0766 mL | 2.1532 mL | 5.3830 mL | |
| 25 mM | 0.1723 mL | 0.8613 mL | 1.7225 mL | 4.3064 mL | |
| 30 mM | 0.1435 mL | 0.7177 mL | 1.4355 mL | 3.5886 mL | |
| 40 mM | 0.1077 mL | 0.5383 mL | 1.0766 mL | 2.6915 mL | |
| 50 mM | 0.0861 mL | 0.4306 mL | 0.8613 mL | 2.1532 mL | |
| 60 mM | 0.0718 mL | 0.3589 mL | 0.7177 mL | 1.7943 mL | |
| 80 mM | 0.0538 mL | 0.2691 mL | 0.5383 mL | 1.3457 mL | |
| 100 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0766 mL |
PF-06840003 Related Classifications
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