TAS0612 (TAS-0612) is an orally bioavailable multikinase inhibitor of AKT, p70S6K, and p90RSK, inhibits Y-box-binding protein (YBX1) phosphorylation.
TAS0612 inhibits cell proliferation and suppresses the phosphorylation of YBX1 in TNBC cell lines, shows antitumor effect against antiestrogen-resistant cells and TNBC cells in vivo.
TAS0612 inhibited pYBX1, pPRAS40 and pS6 in ERα(+)/HER2(−) and ERα(−)/HER2(+) cell lines, the expression levels of pAKT, pp90RSK, and pp70S6K were increased following treatment with relatively higher doses of TAS0612.
TAS0612 showed potent antitumor effects and marked inhibition of pYBX1 and pS6 in the experimental therapeutic model of TNBC.
