PF-06840003

Modify Date: 2024-01-10 06:55:15

Use of PF-06840003

PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.

Name	3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione
Synonym	More Synonyms

Description	PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Indoleamine 2,3-Dioxygenase (IDO) Research Areas >> Cancer
Target	IDO-1
In Vitro	PF-06840003 reverses IDO-1-induced T-cell anergy in vitro[1].
In Vivo	PF-06840003 reduces intratumoral kynurenine levels in mice by >80% and inhibits 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[1].
References	[1]. Tumang J, et al. PF-06840003: a highly selective IDO-1 inhibitor that shows good in vivo efficacy in combination with immune checkpoint inhibitors. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr4863.

Maleimide

CAS#:541-59-3

5-Fluoroindole

CAS#:399-52-0

~38%

PF-06840003

CAS#:198474-05-4

Literature: Henon, Helene; Messaoudi, Samir; Hugon, Bernadette; Anizon, Fabrice; Pfeiffer, Bruno; Prudhomme, Michelle Tetrahedron, 2005 , vol. 61, # 23 p. 5599 - 5614

Precursor 2
CAS#:541-59-3 Maleimide CAS#:399-52-0 5-Fluoroindole
DownStream 0

PF-06840003

PF06840003