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PF-06840003 | IDO1 inhibitor

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

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.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. 2530
3) Blair et al. (2019), IDO1 inhibition potentiates vaccine-induced immunity against pancreatic adenocarcinoma; J. Clin. Invest. 129 1742

PF-06840003 | IDO1 inhibitor is also available in the Cellular Metabolism Library.
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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee