PF-06840003 (Synonyms: EOS200271)

Name: PF-06840003
Brand: MedChemExpress
SKU: HY-101111
Rating: 5.0 (1 reviews)

Cat. No.: HY-101111 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

PF-06840003 Chemical Structure

CAS No. : 198474-05-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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IDO1 IDO2 IDO

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

IDO-1

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

Molecular Weight

232.21

Formula

C₁₂H₉FN₂O₂

CAS No.

198474-05-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.3064 mL	21.5322 mL	43.0645 mL
5 mM	0.8613 mL	4.3064 mL	8.6129 mL
10 mM	0.4306 mL	2.1532 mL	4.3064 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.87%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.3064 mL	21.5322 mL	43.0645 mL	107.6612 mL
	5 mM	0.8613 mL	4.3064 mL	8.6129 mL	21.5322 mL
	10 mM	0.4306 mL	2.1532 mL	4.3064 mL	10.7661 mL
	15 mM	0.2871 mL	1.4355 mL	2.8710 mL	7.1774 mL
	20 mM	0.2153 mL	1.0766 mL	2.1532 mL	5.3831 mL
	25 mM	0.1723 mL	0.8613 mL	1.7226 mL	4.3064 mL
	30 mM	0.1435 mL	0.7177 mL	1.4355 mL	3.5887 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	1.7944 mL
	80 mM	0.0538 mL	0.2692 mL	0.5383 mL	1.3458 mL
	100 mM	0.0431 mL	0.2153 mL	0.4306 mL	1.0766 mL

PF-06840003 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-06840003198474-05-4EOS200271PF06840003PF 06840003EOS 200271EOS-200271Indoleamine 2,3-Dioxygenase (IDO)Inhibitorinhibitorinhibit

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PF-06840003 (Synonyms: EOS200271)

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PF-06840003 Related Antibodies

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References

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PF-06840003 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

PF-06840003 Related Classifications

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