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
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
CAS: 1627856-64-7
Molecular Formula: C22H21F4N3O4
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 - Names and Identifiers
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 - Physico-chemical Properties
| Molecular Formula | C22H21F4N3O4 |
| Molar Mass | 467.41 |
| Density | 1.37±0.1 g/cm3(Predicted) |
| Boling Point | 670.1±55.0 °C(Predicted) |
| Solubility | DMSO : 50 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound p |
| pKa | 10.30±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Use | GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo. GSK3179106 is being developed by GlaxoSmithKline for the treatment of irritable bowel syndrome. GSK3179106 showed IC50s of 0.4 and 11 nM in the biochemical assay and cellular assay, respectively. GSK3179106 had a clean genotoxic profile with no embedded genotoxicity liabilities. |
| Target | RET |
| In vitro study | GSK3179106 is less genotoxic, does not have embedded genetic toxicity, and has good kinase selectivity: in the pool containing more than 300 recombinant kinases, only 26 of these kinases were inhibited by 1 μm GSK3179106. |
| In vivo study | Pharmacokinetic studies were performed in male Sprague-Dawley rats given a single intravenous injection of GSK3179106 at a dose of 0.06 mg/kg: GSK3179106 was low in vivo exposure with an AUC of 102 ng · h/mL. In the in vivo colon allergy model, 7 times (oral) in the first day, oral dose of 10 mg/kg: The results showed that GSK3179106 in the intestinal content, there is a high concentration distribution in the ileum, the concentration is higher than the plasma concentration. |
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 - Reference
| Reference Show more | 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. |
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 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.139 ml | 10.697 ml | 21.394 ml |
| 5 mM | 0.428 ml | 2.139 ml | 4.279 ml |
| 10 mM | 0.214 ml | 1.07 ml | 2.139 ml |
| 5 mM | 0.043 ml | 0.214 ml | 0.428 ml |
Last Update：2024-01-02 23:10:35
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 - Introduction
2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,) isoxazol-3-yl)acetamide inhibitors of tyrosine kinases. It is an organic compound with stable chemical properties.
RET kinase is an important protein kinase involved in the regulation of cell proliferation, differentiation and survival. RET kinase is over-activated in some cancers, leading to tumor initiation and progression. 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,) isoxazol-3-yl)acetamide can selectively inhibit the activity of RET kinase, thus blocking the abnormal signal transduction pathway and inhibiting the growth and spread of tumor.
The preparation of 2-(4-(4-ethoxy-6-oxo-1, 6-dihydrodropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,) isoxazol-3-yl)acetamide usually adopts an organic synthesis method. The specific synthetic route may vary from one research institution or company to another.
RET kinase is an important protein kinase involved in the regulation of cell proliferation, differentiation and survival. RET kinase is over-activated in some cancers, leading to tumor initiation and progression. 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,) isoxazol-3-yl)acetamide can selectively inhibit the activity of RET kinase, thus blocking the abnormal signal transduction pathway and inhibiting the growth and spread of tumor.
The preparation of 2-(4-(4-ethoxy-6-oxo-1, 6-dihydrodropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,) isoxazol-3-yl)acetamide usually adopts an organic synthesis method. The specific synthetic route may vary from one research institution or company to another.
Last Update：2024-04-09 19:05:02
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Product 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 Visit Supplier Webpage Request for quotation
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