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.
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GSK3179106
Dangerous GoodsCAS number：1627856-64-7 molecular formula：C22H21F4N3O4
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | Benzeneacetamide, 4-(4-ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro-N-(5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl)- | DY8BBK4G3C | 1627856-64-7 | HY-100459 | RET Kinase inhibitor 1? | A930132 | 4-(4-Ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro | ||
| CAS number | 1627856-64-7 | molecular formula | C22H21F4N3O4 |
| molecular weight | 467.41 g/mol | Exact mass | 10mM in DMSO |
| PSA | 93.500 Ų | logp | 3.357 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS08
Signal word：
Warning
Hazard Statement：
H361: 怀疑破坏生育力或未出生的孩子
Statement of Preventive Measures：
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。
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MSDS
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