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Product Details

PF-06840003 | IDO1 inhibitor

PF-06840003 (198474-05-4) is a potent (IC50 = 150 and 410 nM via two methods) and selective inhibitor of Indoleamine-2,3-dioxygenase (IDO1).1 In mice with syngeneic tumor grafts, it reduced intratumoral kynurenine levels by over 80%, inhibited tumor growth as monotherapy, and increased the efficacy of anti-PD-L1 therapy.2 PF-06840003 treatment combined with GM-CSF-secreting allogenic pancreatic tumor cell vaccine (GVAX) resulted in increased antitumor efficacy in a murine model of pancreatic ductal adenocarcinoma.3

References/Citations

1) Crosignani et al. (2017), Discovery of a Novel and Selective Indoleamine-2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EROS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate; J. Med. Chem. 60 9617
2) Gomes et al. (2018), Characterization of the Selective Indoleamine-2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy; Mol. Cancer Ther. 9 2530
3) Blair et al. (2019), IDO1 inhibition potentiates vaccine-induced immunity against pancreatic adenocarcinoma; J. Clin. Invest. 129 1742

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Catalog#  10-4498-0005

$60.00
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CAS:
198474-05-4
Catalog Number:
10-4498
Activity:
IDO1 inhibitor/Cancer immunotherapy enhancer
Chemical Name:
3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione
Alternate Name:
EOS200271
Molecular Weight:
232.21
Molecular Formula:
C12H9FN2O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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