| 应用 |
A checkpoint kinase inhibitor for Chk1 and Chk2 |
| 产品介绍 |
AZD7762是Chk1的抑制剂，IC50为5 nM，对Chk2的抑制性与Chk1相近，但对CAM，Yes，Fyn，Lyn，Hck和Lck的抑制性较弱。 |
| 备注 |
AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1. |
| 生化机理 |
AZD-7762 is a novel checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2, respectively. AZD-7762 significantly prolonged the median time required for tumor volume doubling in response to gemcitabine and radiation. Together, findings suggest that G(2) checkpoint abrogation and homologous recombination repair inhibition both contribute to sensitization by Chk1 inhibition. Furthermore, they support the clinical use of AZD-7762 in combination with gemcitabine and radiation for patients with locally advanced pancreatic cancer. |
| 别名 |
AZD7762; AZD 7762; 5-(3-氟苯基)-3-脲基噻吩-N-((S)-哌啶-3-基)-2-甲酰胺;;AZD7762;AZD 7762;5-(3-fluorophenyl)-3-ureidothiophene-n-((s)-piperidin-3-yl)-2-carboxamide;1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea |
