GNE-0877
| CAS号 | 1374828-69-9 | 货号 | BCP09654 |
| 中文名 | GNE-0877 | ||
| 英文名 | GNE-0877 | ||
| 中文别名 | |||
| 英文别名 | GNE 0877;GNE0877; | ||
| 分子式 | C14H16F3N7 | 分子量 | 339.32 |
| 生物活性 | Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in the maintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension. | ||
| 信号通路 | Others Pathway | ||
| 靶 点 | LRRK2 | ||
结构式
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