3-Quinolinecarboxylic acid, 6-[[(2S)-2-[([1,1'-biphenyl]-4-ylcarbonyl)amino]-1-oxopropyl]amino]-1,4-dihydro-4-oxo-

Biological Activity

PTPN22-IN-1 is a potent PTPN22 inhibitor (IC50=1.4 μM; Ki=0.50 μM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses[1]. From WO2021007491A1 compound L-1. PTPN22-IN-1 (Compound L-1) (WT mice; intraperitoneally) significantly reduces MC38 tumor growth. PTPN22-IN-1 (syngeneic immunocompetent model; CT26 in Balb/c mice) shows similar antitumor effects[1].Administration of L-l intraperitoneally at 10 mg/kg yielded an average AUC of 4.55 μM h and Cmax of 1.1 1 μM (Fig. 9d), which is more than twice of its Ki value[1]. PTPN22-IN-1 (Compound L-1) (WT mice; intraperitoneally) significantly reduces MC38 tumor growth. PTPN22-IN-1 (syngeneic immunocompetent model; CT26 in Balb/c mice) shows similar antitumor effects[1].Administration of L-l intraperitoneally at 10 mg/kg yielded an average AUC of 4.55 μM h and Cmax of 1.1 1 μM (Fig. 9d), which is more than twice of its Ki value[1].

References

[1]. Elizabeth Jaffee, et al. Targeting ptpn22 in cancer therapy. WO2021007491A1.