Art. -Nr.: HY-101111

PF-06840003

(Synonyms: EOS200271)

1 Cited Publications

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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.

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Reinheit: 99.87%
CAS. Nr.: 198474-05-4
Formel: C₁₂H₉FN₂O₂
Molecular Weight:232.21

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-06840003 Chemical Structure

CAS. Nr.: 198474-05-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

IDO-1

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	0.21 μM Compound: PF-06840003	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	[PMID: 30469041]
HeLa	IC₅₀	1.8 μM Compound: 6; EOS200271; PF-06840003	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	[PMID: 29111717]

In Vitro

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.

In Vivo

PF-06840003 reduces intratumoral kynurenine levels in mice by >80% and inhibits tumor growth in multiple preclinical syngeneic models in mice, in combination with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 198474-05-4
Appearance Solid
Molecular Weight 232.21
Formel C₁₂H₉FN₂O₂
Color Light yellow to yellow
SMILES

O=C(C(C1=CNC2=C1C=C(F)C=C2)C3)NC3=O
Synonyms

EOS200271
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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Cell Chem Biol

DELs enable the development of BRET probes for target engagement studies in cells. [Abstract]

2023 Aug 17;30(8):987-998.e24. PMID: 37490918

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3064 mL

21.5319 mL

43.0637 mL

5 mM

0.8613 mL

4.3064 mL

8.6127 mL

10 mM

0.4306 mL

2.1532 mL

4.3064 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tumang J, et al. PF-06840003: a highly selective IDO-1 inhibitor that shows good in vivo efficacy in combination with immune checkpoint inhibitors. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr4863.

[2]. Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate. J Med Chem. 2017 Dec 14;60(23):9617-9629. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PF-06840003

1 Cited Publications

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PF-06840003

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

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MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) PF-06840003

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06840003

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) PF-06840003

Alle Indoleamine 2,3-Dioxygenase (IDO) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06840003 Related Classifications

HY-101111 Related Classifications