GSK3179106

1627856-64-7

C22H21F4N3O4

DMSO : >= 100 mg/mL (213.94 mM)

Protein Tyrosine Kinase/RTK

GSK3179106 is a potent and selective RET kinase inhibitor with an IC₅₀ of 0.4 nM^[1]. IC50 & Target: IC50: 0.4+/-0.2 nM (Human RET), 0.2+/-0.1 nM (Rat RET)^[1] In Vitro: GSK3179106 (10 nM-100 uM; 8 days for TT cells, 3 days for SK-N-AS and A549 cells) inhibits the proliferation of the RET-dependent TT cell line with a mean IC₅₀ value of 25.5 nM however has no effect on the proliferation of the RET-independent SK-NAS and A549 cell lines (mean IC₅₀>10 uM and IC₃₀>17 uM, respectively)^[1].
GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC₅₀s of 4.6 nM and 11.1 nM, respectively^[1]. In Vivo: 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^[1].