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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; | ||
SMILES | |||
化学名称 | |||
分子式 | C14H16F3N7 | 分子量 | 339.32 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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. |
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