10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
🌡
Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
📋
Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
📚
Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
Information
GSK3179106 GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.
Targets
RET (Cell-free assay) 0.3 nM
In vitro
GSK3179106 has a clean genotoxic profile with no embedded genotoxicity liabilities and possesses good kinase selectivity: only 26 out of a set of >300 recombinant kinases are found to be inhibited at a 1 μM test concentration.
In vivo
Single dose IV (bolus, 0.06 mg/kg) PK in male Sprague-Dawley rats of compound GSK3179106 formulated as 0.04 mg/mL in DMSO/6% HP-beta-CD = 5:95 with a pH of 7 as a clear solution shows low exposure with an AUC of 102 ng·h/mL. Oral PK is evaluated with the same dosing regimen as the in vivo colonic hypersensitivity model, seven doses of 10 mg/kg given over 3.5 days. Full gut PK measurements are also taken to help understand the PK/PD relationship--It reveals high concentrations of GSK3179106 in the colon contents, jejunum, duodenum, and ileum, over that in plasma.
GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
This compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
We use cookies to ensure the website functions properly and, where permitted, to improve your experience. You can manage your preferences at any time in Settings. Learn more in our Cookie Policy.
Shall we send you a message when we have discounts available?
Remind me later
Thank you! Please check your email inbox to confirm.
Products are supplied to verified businesses, institutions, and qualified professionals for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
