GSK3179106 (Synonyms: RET Kinase Inhibitor 1) |
| Katalog-Nr.GC18492 |
GSK3179106 ist ein oral aktiver und selektiver RET-Kinase-Inhibitor mit IC50-Werten von 0,4 nM, 0,2 nM fÜr Human-RET bzw. Ratten-RET.
Products are for research use only. Not for human use. We do not sell to patients.
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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