GSK3179106 是选择性的、具有口服活性的RET激酶抑制剂，对人和大鼠 RET 的 IC50 分别为 0.4 nM 和 0.2 nM。它能够减轻炎症后和应激引起的内脏超敏反应，对肠易激综合征具有潜在的应用价值。

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

The effect of GSK3179106 on human and rat RET enzymatic activity and motesanib on human RET enzymatic activity was determined in an in vitro biochemical homogeneous time-resolved fluorescence (HTRF) assay.

GSK3179106 (3 or 10 mg/kg; orally; for 3.5 days BID) reduces the visceromotor response (VMR) in comparison to rats given an acetic acid enema and dosed with vehicle.

1627856-64-7

C22H21F4N3O4

467.421

DMSO:100 mg/mL (213.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years