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Pack Size | Price | Availability | Quantity |
---|---|---|---|
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 |
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 |
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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (258.39 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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