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编 号:F752070
分子式:C26H26ClN7O9
分子量:615.98
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生物活性:
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. CD73-IN-14 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
CD73-IN-14 (10, 25, 50 mg/kg; p.o.; twice-a-day for 20 days) shows anti-tumor activity in mouse.br/>Pharmacokinetic Parameters of CD73-IN-14 in rats.PO Dose (mg/kg)AUC0-24 h (ng*hr/mL) Cmax(nM)Tmax(hr)
50580740.8
200609418000.8
50018500110000.3
rats, 50, 200, 500 mg/kg p.o.Animal Model:C57BL/6 mice (EG7 model)
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.
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