TAS0728

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors^[1]. IC50 & Target:IC50: 13 nM (HER2), 4.9 nM (BMX), 8.5 nM (HER4), 31 nM (BLK), 65 nM (EGFR), 33 nM (JAK3), 25 nM (SLK), 86 nM (LOK), 36 nM (Human HER2)^[1] In Vitro: TAS0728 is a covalent-binding inhibitor of HER2 kinase and exhibits high selectivity for HER2 kinase. It also shows inhibitory activity against BMX, HER4, BLK, EGFR, JAK3, SLK, and LOK^[1]. In Vivo: TAS0728 reveals the sustained and targeted inhibition of phosphorylation of HER2, HER3, AKT and ERK. TAS0728 also shows the ability of tumor regression and low toxicity^[1].