| 应用 |
A selective NPM-ALK phosphorylation inhibitor which also inhibits ALK and LRRK2 Kinase |
| 产品介绍 |
TAE684 (NVP-TAE684)是一种有效的，选择性的ALK抑制剂，IC50为3 nM，作用于ALK比作用于InsR选择性高100倍。 |
| 备注 |
TAE684 is a potent and selective ALK inhibitor with IC50 of 3 nM, 100-fold more sensitive for ALK than InsR. |
| 生化机理 |
TAE684 selectively inhibits the phosphorylation of NPM-ALK, inducing apoptosis and G1 phase arrest in Ba/F3 cell lines. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. |
| 别名 |
NVP-TAE684; 5-氯-N2-[2-甲氧基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-N4-[2-[(1-甲基乙基)磺酰基]苯基]-2,4-嘧啶二胺;5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine; NVP-TAE684 |
