TAS0728 是一种 HER2 抑制剂，与HER2的 C805 位点共价结合，IC50值为 13 nM。它抑制 HER2、HER3 及其下游效应蛋白的磷酸化，具有抗肿瘤活性。

TAS0728 is a HER2 inhibitor, with antitumor activity

TAS0728 exhibited robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis of HER2-amplified breast cancer cells and in tumor tissues of a xenograft model.?TAS0728 induced tumor regression in mouse xenograft models bearing HER2 signal-dependent tumors and exhibited a survival benefit without any evident toxicity in a peritoneal dissemination mouse model bearing HER2-driven cancer cells[1].

2088323-16-2

C26H32N8O3

504.595

DMSO:125 mg/mL (247.73 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years