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
Biochemicals & reagents
198474-05-4
EOS200271
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
-20°C
TARGET: Tryptophan -- PATHWAY: Amino acid metabolism; IDO/TDO pathways -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer