Cas No.: | 198474-05-4 |
Synonyms: | PF 06840003,PF-06840003 |
SMILES: | C1C(C(=O)NC1=O)C2=CNC3=C2C=C(C=C3)F |
Formula: | C12H9FN2O2 |
M.Wt: | 232.21 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor. |
Target: | IDO-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]. |
In Vitro: | PF-06840003 reverses IDO-1-induced T-cell anergy in vitro[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. |