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PF-06840003

Catalog No. T4307 CAS 198474-05-4

Synonyms: EOS200271, PF 06840003

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PF-06840003, CAS 198474-05-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 85.00
25 mg	In stock	$ 133.00
50 mg	In stock	$ 182.00
100 mg	In stock	$ 288.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.89%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Synonyms	EOS200271, PF 06840003
Molecular Weight	232.21
Formula	C12H9FN2O2
CAS No.	198474-05-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (258.39 mM)

References and Literature

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. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin resistant lung cancer[J]. Molecular Cancer Research. 2019: molcanres. 0239.2019. 3. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin-resistant lung cancer[J]. Molecular Cancer Research. 2020, 18(1): 105-117.

Citations

1. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin resistant lung cancer. Molecular Cancer Research. 2019: molcanres. 0239.2019

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Clinical Compound Library Anti-Cancer Metabolism Compound Library Target-Focused Phenotypic Screening Library Anti-Metabolism Disease Compound Library

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IDO1-IN-1 IDO-IN-8 IDO-IN-12 IDO1-IN-5 IACS-8968 R-enantiomer Epacadostat β-Lapachone IDO-IN-11

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-06840003 198474-05-4 Metabolism IDO Indoleamine 2,3-Dioxygenase (IDO) EOS-200271 EOS200271 PF 06840003 inhibit Inhibitor PF06840003 EOS 200271 inhibitor

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