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PF-06840003

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Purity:99.89%

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COA HPLC HNMR LCMS

PF-06840003

Catalog No. T4307Cas No. 198474-05-4

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

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Pack Size	Price	Availability
2 mg	$38	In Stock
5 mg	$61	In Stock
10 mg	$85	In Stock
25 mg	$133	In Stock
50 mg	$182	In Stock
100 mg	$288	In Stock
1 mL x 10 mM (in DMSO)	$108	In Stock

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Product Introduction

Bioactivity

Description	PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor.
Targets&IC50	IDO1 (mouse):1.5 μM, dIDO1:0.59 μM, IDO1 (human):0.41 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.
Alias	EOS200271, PF 06840003

Chemical Properties

Molecular Weight	232.21
Formula	C12H9FN2O2
Cas No.	198474-05-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 60 mg/mL (258.39 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.3064 mL	21.5322 mL	43.0645 mL	215.3223 mL
5 mM	0.8613 mL	4.3064 mL	8.6129 mL	43.0645 mL
10 mM	0.4306 mL	2.1532 mL	4.3064 mL	21.5322 mL
20 mM	0.2153 mL	1.0766 mL	2.1532 mL	10.7661 mL
50 mM	0.0861 mL	0.4306 mL	0.8613 mL	4.3064 mL
100 mM	0.0431 mL	0.2153 mL	0.4306 mL	2.1532 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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