TAS0728

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TAS0728

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
5mg	询价
10mg	询价

TAS0728 是一种有效、选择性、可口服、不可逆、共价结合的 HER2 抑制剂，与 HER2 的 C805 位点共价结合，抑制其活性，IC50 值为 13 nM。TAS0728 对 BMX，HER4，BLK，EGFR，JAK3，SLK，LOK 和人 HER2 的 IC50 值分别为 4.9，8.5，31，65，33，25，86 和 36 nM。TAS0728 同时可抑制 HER2，HER3 及其下游效应蛋白的磷酸化。具有抗肿瘤活性。

HER4

8.5nM(IC₅₀)

HER2

13nM(IC₅₀)

HumanHER2

36nM(IC₅₀)

EGFR

65nM(IC₅₀)

产品描述

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].

[1]. Irie H, et al. TAS0728, a covalent-binding, HER2-selective kinase inhibitor shows potent antitumor activity in preclinical models. Mol Cancer Ther. 2019 Feb 20.