TAS0728 |
Catalog No.GC65310 |
TAS0728 es un inhibidor de HER2 potente, selectivo, activo por vÍa oral, irreversible y de uniÓn covalente, con una IC50 de 13 nM. TAS0728 también muestra IC50 de 4.9, 8.5, 31, 65, 33, 25 y 86 nM para BMX, HER4, BLK, EGFR, JAK3, SLK y LOK respectivamente. AdemÁs, TAS0728 exhibe una inhibiciÓn sÓlida y sostenida de la fosforilaciÓn de HER2
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Cas No.: 2088323-16-2
Sample solution is provided at 25 µL, 10mM.
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.
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