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。
货号:ajcx39330
CAS:2088323-16-2
分子式:C26H32N8O3
分子量：504.58
溶解度:DMSO : 125 mg/mL (247.73 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

Protocol:

HER4 8.5nM(IC50)

HER2 13nM(IC50)

HumanHER2 36nM(IC50)

EGFR 65nM(IC50)

BMX 4.9nM(IC50)

BLK 31nM(IC50)

JAK3 33nM(IC50)

SLK 25nM(IC50)

LOK 86nM(IC50)