| 应用 |
A potent, selective, small-molecule tyrosine kinase HER2 inhibitor |
| 产品介绍 |
这个产品是ARRY-380的类似物, ARRY-380是高活性HER2抑制剂，IC50为8 nM，对剪切型p95-HER2有相同的抑制性，比对EGFR的抑制性高500倍。 |
| 备注 |
ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. Phase 1. |
| 生化机理 |
ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation. |
| 别名 |
ARRY380; ARRY 380; 6-[5-[[[2-(甲磺酰基)乙基]氨基]甲基]-2-呋喃基]-N-[3-甲基-4-([1,2,4]三唑并[1,5-a]吡啶-7-氧基)苯基]-4-氨基喹唑啉;ARRY380;ARRY 380; 6-[5-[[[2-(Methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4-quinazolinamine |
