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PF-06840003

SKU: orb1302966

Description

PF-06840003 (EOS200271) is a potent and selective small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with oral bioavailability. It is a research tool used in immuno-oncology to study IDO1's role in tryptophan metabolism and immune suppression in both cellular assays and in vivo models.

Research Area

Metabolism Research

Images & Validation

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PF-06840003

Key Properties

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CAS Number198474-05-4
MW232.21
Purity99.89% (May vary between batches)
FormulaC12H9FN2O2
SMILESFc1ccc2[nH]cc(C3CC(=O)NC3=O)c2c1
TargetIndoleamine 2,3-Dioxygenase (IDO),IDO
SolubilityDMSO:60 mg/mL (258.39 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.61 mM)

Bioactivity

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Target IC50
IDO1 (human):0.41 μM|IDO1 (mouse):1.5 μM|dIDO1:0.59 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.
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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).
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Indoleamine2,3Dioxygenase(IDO), Indoleamine 2,3Dioxygenase (IDO), Indoleamine 2,3-Dioxygenase (IDO), Indoleamine2,3Dioxygenase, Indoleamine 2,3-Dioxygenase, inhibit, EOS 200271, EOS200271, EOS-200271, Inhibitor, IDO1, IDO, PF06840003, PF-06840003, PF 06840003

Similar Products

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  • PF-06840003

    PF-06840003 [orb1225770]

    >98% (HPLC)

    198474-05-4

    232.2104632

    C12H9FN2O2

    1 g, 500 mg, 200 mg, 25 mg, 2 mg, 50 mg, 5 mg, 10 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
23063810 ↗

Key Properties

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No computed properties available.

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PF-06840003 (orb1302966)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 70.00
5 mg
$ 90.00
1 ml x 10 mM (in DMSO)
$ 100.00
10 mg
$ 130.00
25 mg
$ 160.00
50 mg
$ 180.00
100 mg
$ 260.00
200 mg
$ 370.00
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