TAS0728
| CAS No. | 2088323-16-2 | Cat. No. | BCP33300 |
| Name | TAS0728 | ||
| Synonyms | TAS-0728; TAS 0728; | ||
| Formula | C26H32N8O3 | M. Wt | 504.6 |
| Description | TAS0728 is a potent, selective, covalent, orally active HER2 inhibitor with IC50 of 36 nM. TAS0728 bound to HER2 kinase, the inhibitory activity was not affected by a high ATP concentration. TAS0728 exhibited robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis of HER2-amplified breast cancer cells and in tumor tissues of a xenograft model. TAS0728 induced tumor regression in mouse xenograft models bearing HER2 signal-dependent tumors and exhibited a survival benefit without any evident toxicity in a peritoneal dissemination mouse model bearing HER2-driven cancer cells. | ||
| Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
| Targets | EGFR | ||
Structure
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