| Name | PF-06840003 |
| Description | PF-06840003 (EOS200271) is a specific and orally active IDO-1 inhibitor. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (8.61 mM), Sonication is recommended.
DMSO : 60 mg/mL (258.39 mM), Sonication is recommended.
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| Keywords | PF-06840003 | PF06840003 | Inhibitor | inhibit | Indoleamine2,3Dioxygenase(IDO) | Indoleamine2,3Dioxygenase | Indoleamine 2,3-Dioxygenase (IDO) | Indoleamine 2,3Dioxygenase (IDO) | Indoleamine 2,3-Dioxygenase | IDO1 | IDO | EOS-200271 | EOS 200271 |
| Inhibitors Related | Palmatine chloride | GNF-PF-3777 | Necrostatin-1 | IDO-IN-7 | TDO-IN-1 | IDO1-IN-28 | Indoximod | Palmatine | Epacadostat | β-Lapachone | IDO-IN-12 | 3-TYP |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
