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编 号:F715360
分子式:C15H17FN6O4
分子量:364.33
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生物活性:
IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.

体内研究:
IDO1-IN-2 (100 mg/kg, twice daily) demonstrates good efficacy synergy when combined with anti-PD-1 mAb in a mouse EMT6 tumor syngeneic model. IDO1-IN-2 has a t1/2 of 3.7 hours, a CL/CLu of 15/319 mL/min/kg, and a F of 63% for rats. IDO1-IN-2 has a t1/2 of 6 hours, a CL/CLu of 6/88 mL/min/kg, and a F of 67% for dogs.

体外研究:
IDO1-IN-2 inhibits amino-cyclobutarene-derived indoleamine-2,3-dioxygenase 1 (IDO1) Hela cellular with an IC50 of 49 nM. IDO1-IN-2 has an IC50 of 249 nM for IDO1 wholr blood.
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