CD73-IN-14

D73-IN-14 is a potent, selective and orally active CD73 inhibitor with an IC50 value of 0.17 nM. CD73-IN-14 increases the number of tumor-infiltrating CD8+ cells and shows anti-tumor activity[1].

Research Areas >> Cancer

C50: 0.17 nM (CD73)[1]

CD73-IN-14 (10, 25, 50 mg/kg; p.o.; twice-a-day for 20 days) shows anti-tumor activity in mouse[1].br/>Pharmacokinetic Parameters of CD73-IN-14 in rats[1]. PO Dose (mg/kg) AUC0-24 h (ng*hr/mL) Cmax(nM) Tmax(hr) 50 580 74 0.8 200 6094 1800 0.8 500 18500 11000 0.3 rats, 50, 200, 500 mg/kg p.o.[1] Animal Model: C57BL/6 mice (EG7 model)[1] Dosage: 10, 25, 50 mg/kg Administration: P.o.; twice a day for 20 days Result: Increased tumor-infiltrating CD8+ cells and decreased the tumor volume in a dose dependet manner.

[1]. Li J, et al. Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates In Vivo Antitumor Activity. J Med Chem. 2022 Dec 18.