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Chemical Structure : GSK3179106
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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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
| M.Wt | 467.421 | |
| Formula | C22H21F4N3O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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