TAS0728 |
| رقم الكتالوجGC65310 |
TAS0728 هو مثبط HER2 قوي ، انتقائي ، فعال عن طريق الفم ، لا رجعة فيه ، ملزم تساهمي ، مع IC50 من 13 نانومتريُظهر TAS0728 أيضًا IC50s من 4.9 و 8.5 و 31 و 65 و 33 و 25 و 86 نانومتر لـ BMX 、 HER4 、 BLK 、 EGFR 、 JAK3 、 SLK و LOK على التواليعلاوة على ذلك ، يُظهر TAS0728 تثبيطًا قويًا ومستدامًا للفسفرة لـ HER2
Products are for research use only. Not for human use. We do not sell to patients.
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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