PTPN22-IN-1

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.

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

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].

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