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Background Information:
PF-06840003 (EOS-200271) is a highly selective, orally bioavailable and neuroactive IDO-1 inhibitor. PF-06840003 reversed IDO-1-induced T-cell anergy in vitro. In vivo, PF-06840003 reduced intratumoral kynurenine levels in mice by >80% and inhibited tumor growth in multiple preclinical syngeneic models in mice, in combination with immune checkpoint inhibitors. PF-0684003 has favorable predicted human pharmacokinetic properties, including a predicted t1/2 of 16-19 hours (refs. 1, 2). It is currently in clinical evaluation.
Reference:
1. J. Tumang, et al, PF-06840003: a highly selective IDO-1 inhibitor that shows good in vivo efficacy in combination with immune checkpoint inhibitors, Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. AACR; Cancer Res 2016;76(14 Suppl):Abstract nr4863.
2. David Reardon, et al, ATIM-29. A PHASE 1 STUDY OF PF-06840003, AN ORAL INDOLE 2,3-DIOXYGENASE 1 (IDO1) INHIBITOR IN PATIENTS WITH MALIGNANT GLIOMAS, Neuro-Oncology, Volume 19, Issue suppl_6, 6 November 2017, Pages vi32.
APIM050368: PF-06840003 (EOS-200271)
CAS No.: 198474-05-4.
Molecular Formula: C12H9FN2O2.
Molecular Weight: 232.2 (or refer to Certificate of Analysis, batch-specific).
Purity: >99.5% by HPLC (at 254 nm).
QC: HPLC-MS, 1H-NMR, Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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