GSK3179106 (Synonyms: RET Kinase Inhibitor 1) |
| Catalog No.GC18492 |
GSK3179106 est un inhibiteur de kinase RET actif et sélectif par voie orale avec des IC50 de 0,4 nM, 0,2 nM pour le RET humain et le RET de rat, respectivement.
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Cas No.: 1627856-64-7
Sample solution is provided at 25 µL, 10mM.
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GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM[1].
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)[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].
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].
References:
[1]. Russell JP, et al. Exploring the Potential of RET Kinase Inhibition for Irritable Bowel Syndrome: A Preclinical Investigation in Rodent Models of Colonic Hypersensitivity. J Pharmacol Exp Ther. 2019 Feb;368(2):299-307.
[2]. Russell JP, et al. Enteric RET inhibition attenuates gastrointestinal secretion and motility via cholinergic signaling in rat colonic mucosal preparations. Neurogastroenterol Motil. 2019 Apr;31(4):e13479.
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