1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)
  3. PF-06840003

PF-06840003 (Synonyms: EOS200271)

Cat. No.: HY-101111 Purity: 99.79%
Handling Instructions

PF-06840003 is a highly selective orally bioavailable 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

PF-06840003 Chemical Structure

CAS No. : 198474-05-4

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 128 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
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50 mg USD 220 In-stock
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100 mg USD 350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor[1] with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively[2].

IC50 & Target[1]

IDO-1

 

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].

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].

Clinical Trial
Molecular Weight

232.21

Formula

C₁₂H₉FN₂O₂

CAS No.

198474-05-4

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (430.64 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Product Name:
PF-06840003
Cat. No.:
HY-101111
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