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PF-06840003

Chemical Structure : PF-06840003

CAS No.: 198474-05-4

PF-06840003 (PF06840003;PF 06840003;EOS 200271)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-06840003 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.

Physicochemical Properties

M.Wt 232.2104632
Formula C12H9FN2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

2,5-Pyrrolidinedione, 3-(5-fluoro-1H-indol-3-yl)-

References

1. Crosignani S, et al. J Med Chem. 2017 Nov 21. doi: 10.1021/acs.jmedchem.7b00974.

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