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GSK3179106

Chemical Structure GSK3179106

CAS No.: 1627856-64-7

GSK3179106 (GSK 3179106;GSK-3179106)

Catalog No.: PC-35286Not For Human Use, Lab Use Only.

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted RET kinase inhibitor with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively, 273-fold selectivity over KDR.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted RET kinase inhibitor with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively, 273-fold selectivity over KDR; possesses good kinase selectivity, only 26 out of a set of >300 recombinant kinases were found to be inhibited at 1 uM; GSK3179106 dosed orally at 10 mg/kg for 3.5 days BID reduced the visceromotor response to colorectal distension in comparison to rats given an acetic acid enema and dosed with vehicle, GSK3179106 has been developed for the treatment of IBS in a clinical setting.

Irritable Bowel Syndrome

Phase 1 Clinical

Physicochemical Properties

M.Wt 467.421
Formula C22H21F4N3O4
CAS No. 1627856-64-7
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name

2-[4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl]-N-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl]acetamide

Clinical Information

References

1. Hilary Schenck Eidam, et al. Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS. ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.8b00035.

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