| Description |
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[1].
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| Related Catalog |
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| Target |
IDO1:81 nM (IC50)
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| In Vitro |
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[1].
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| In Vivo |
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[1]. 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[1].
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| References |
[1]. Zhang H, et al.Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536.
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