CD161

CD161 is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity^[1]. IC50 & Target:IC50: 28.2 nM (BRD4 BD1) and 7.2 nM (BRD4 BD2)^[1] In Vitro: CD161 has K_is of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively^[1].
CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner^[1].
In Vivo: CD161 (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition^[1].
CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t_1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the C_max of 7333 ng/mL (po) for rat. The t_1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the C_max of mice is 983.1 ng/mL (po) ^[1].