GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

RET Kinase inhibitor 1

DMSO : ≥ 100 mg/mL (213.94 mM)

GSK3179106 (10 nM-100 µM; 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 µM and IC30>17 µM, respectively).GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC50s of 4.6 nM and 11.1 nM, respectively.Cell Viability AssayCell Line:TT, SK-N-AS and A549 cellsConcentration:10 nM-100 µMIncubation Time:8 days for TT cells, 3 days for SK-N-AS and A549 cellsResult:Inhibited the proliferation of TT cell line with a mean IC50 value of 25.5 nM however had no effect on the proliferation of the SK-NAS and A549 cell lines (mean IC50>10 µM and IC30>17 µM, respectively).

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.