| Bioactivity | 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. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | PTPN22-IN-1 | ||||||||||||
| CAS | 2580935-57-3 | ||||||||||||
| Formula | C26H21N3O5 | ||||||||||||
| Molar Mass | 455.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Elizabeth Jaffee, et al. Targeting ptpn22 in cancer therapy. WO2021007491A1. |