CQ211 is a potent and selective RIOK2 inhibitor with a K d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines [1].
In Vivo, CQ211 (25 mg/kg; i.p; for 18 consecutive days; once daily) inhibits MKN-1 xenograft mouse model[1].
In Vitro, CQ211 (0-5.0 μM; 4 h) suppresses the phosphorylation of mTOR in cancer cells[1]. CQ211 can obviously suppress the proliferation of MKN-1 and HT-29 cells with IC50 values of 0.61 μM and 0.38 μM, respectively[1].
References:
[1]. Ouyang Y, et al. Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. J Med Chem. 2022 Jun 9;65(11):7833-7842.
In Vivo, CQ211 (25 mg/kg; i.p; for 18 consecutive days; once daily) inhibits MKN-1 xenograft mouse model[1].
In Vitro, CQ211 (0-5.0 μM; 4 h) suppresses the phosphorylation of mTOR in cancer cells[1]. CQ211 can obviously suppress the proliferation of MKN-1 and HT-29 cells with IC50 values of 0.61 μM and 0.38 μM, respectively[1].
References:
[1]. Ouyang Y, et al. Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. J Med Chem. 2022 Jun 9;65(11):7833-7842.