TAS0728 |
| Catalog No.GC65310 |
TAS0728은 IC50이 13nM인 강력하고 선택적인 경구 활성, 비가역적 공유 결합 HER2 억제제입니다. TAS0728은 또한 BMX, HER4, BLK, EGFR, JAK3, SLK 및 LOK에 대해 각각 4.9, 8.5, 31, 65, 33, 25 및 86nM의 IC50을 보여줍니다. 또한, TAS0728은 HER2
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Cas No.: 2088323-16-2
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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