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Chemical Structure : PF-06840003
CAS No.: 198474-05-4
Catalog No.: PC-42320Not For Human Use, Lab Use Only.
PF-06840003 is a novel potent, selective, orally active, and CNS penetrant IDO-1 inhibitor with IC50 of 0.41 uM for hIDO-1.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $58 | In stock | |
| 10 mg | $88 | In stock | |
| 25 mg | $138 | In stock | |
| 50 mg | $228 | In stock | |
| 100 mg | $388 | In stock | |
| 250 mg | Get quote |
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PF-06840003 (EOS200271) is a novel potent, selective, orally active, and CNS penetrant IDO-1 inhibitor with IC50 of 0.41 uM for hIDO-1.
PF-06840003 weakly inhibits hTDO-2 with IC50 of 140 uM, and shows no activity against hIDO-2 (>100 uM).
PF-06840003 shows activity both in the HeLa assay (IC50=1.8 uM) as well as in the LPS/INFγ-stimulated THP1 cells (IC50=1.7 uM), maintains good efficiency in the whole blood assay (IC50=4.7 uM).
PF-06840003 shows significant antitumor activity in mice and very favorable ADME profile.
| M.Wt | 232.2104632 | |
| Formula | C12H9FN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 28 mg/mL |
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| Chemical Name/SMILES |
2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)- |
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1. Crosignani S, et al. J Med Chem. 2017 Nov 21. doi: 10.1021/acs.jmedchem.7b00974.
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