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Product Infomation
Product NameGSK3179106
CAS No.1627856-64-7
Molecular Weight

467.41

Formula

C₂₂H₂₁F₄N₃O₄

SMILES

O=C(NC1=NOC(C(C)(C)C(F)(F)F)=C1)CC2=CC=C(C(C(OCC)=C3)=CNC3=O)C=C2F

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Product description

Description

GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity[1].


IC50 & Target

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IC50: 0.4 nM (human RET), 0.2 nM (rat RET)[1]


In Vitro

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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].







Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

 [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.