首页 蛋白库 基因库 产品 会员服务
位置：首页 > 产品库 > GSK3179106
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
GSK3179106
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。
GSK3179106图片
CAS NO:1627856-64-7
包装与价格：
包装价格(元)
1mg询价
5mg询价
10mg询价
25mg询价

GSK3179106 是一种具有口服活性的选择性 RET 激酶抑制剂，对人 RET 和大鼠 RET 的 IC50 分别为 0.4 nM 和 0.2 nM。
Cas No.1627856-64-7
化学名4-(4-ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro-N-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-benzeneacetamide
Canonical SMILESO=C1C=C(OCC)C(C2=CC(F)=C(CC(NC3=NOC(C(C)(C)C(F)(F)F)=C3)=O)C=C2)=CN1
分子式C22H21F4N3O4
分子量467.4
溶解度DMSO : 100 mg/mL (216.57 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.

 
 
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024