PTPN22-IN-1 is a potent PTPN22 inhibitor (IC 50 =1.4 μM; K i =0.50 μM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses. From WO2021007491A1 compound L-1.
性状
Solid
体外研究(In Vitro)
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.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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
Administration of L-l intraperitoneally at 10 mg/kg yielded an average AUC of 4.55 μM h and C max of 1.1 1 μM (Fig. 9d), which is more than twice of its K i value. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Elizabeth Jaffee, et al. Targeting ptpn22 in cancer therapy. WO2021007491A1.
溶解度数据
In Vitro: DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)