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RET Kinase Inhibitor 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RET Kinase Inhibitor 1图片
CAS NO:1627856-64-7
规格:98%
分子量:467.4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
C22H21F4N3O4
CAS:1627856-64-7
分子式:C22H21F4N3O4
分子量:467.4
纯度:98%
存储:Store at -20°C

Background:

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM[1].


GSK3179106 (10 nM-100 μM; 8 days for TT cells, 3 days for SK-N-AS and A549 cells) inhibits the proliferation of the RET-dependent TT cell line with a mean IC50 value of 25.5 nM however has no effect on the proliferation of the RET-independent SK-NAS and A549 cell lines (mean IC50>10 μM and IC30>17 μM, respectively)[1].GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC50s of 4.6 nM and 11.1 nM, respectively[1].


GSK3179106 (3 or 10 mg/kg; orally; for 3.5 days BID) reduces the visceromotor response (VMR) in comparison to rats given an acetic acid enema and dosed with vehicle[1].


参考文献:
[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.