GSK3179106 (Standard)

GSK3179106 (Standard) is the analytical standard of GSK3179106 (HY-100459) . This product is intended for research and analytical applications. 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].

Product Specifications

CAS Number

[1627856-64-7]

Target

Reference Standards; RET

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Field of Research

Metabolic Disease; Inflammation/Immunology

Smiles

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

Molecular Formula

C22H21F4N3O4

Molecular Weight

467.41

References & Citations

[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.