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首页-小分子抑制剂&激动剂-Tyrosine Kinase-RET Tyrosine Kinase (c-RET)-GSK3179106
GSK3179106

Chemical Structure : GSK3179106

CAS No.: 1627856-64-7

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GSK3179106 (GSK 3179106, GSK-3179106)

货号: 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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10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
GSK3179106 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.

物理化学性质&存储条件

分子量 467.421
分子式 C22H21F4N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

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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