货号	规格	价格	上海	北京	珠海	重庆	武汉
S83738-5mg	99.30%	￥269.00 S83738-5mg ￥269.00 现货	5 5	-	-	-	-
S83738-10mg促销	99.30%	￥570.00 ￥456.00 S83738-10mg ￥456.00 现货	5 5	-	-	-	-
S83738-25mg	99.30%	￥824.00 S83738-25mg ￥824.00 现货	5 5	-	-	-	-
S83738-100mg	≥99%	￥2800.00 S83738-100mg ￥2800.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity

靶点：

IC50: 0.4 nM (human RET), 0.2 nM (rat RET);c-RET

体外研究：

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).
GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC50s of 4.6 nM and 11.1 nM, respectively. Cell Viability Assay Cell Line: TT, SK-N-AS and A549 cells Concentration: 10 nM-100 µM Incubation Time: 8 days for TT cells, 3 days for SK-N-AS and A549 cells Result: Inhibited the proliferation of TT cell line with a mean IC50 value of 25.5 nM however had no effect on the proliferation of the SK-NAS and A549 cell lines (mean IC50>10 µM and IC30>17 µM, respectively).

体内研究：

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. Animal Model: Seventy male Sprague Dawley rats (225-250 g, ~7-8 weeks old); Fifty male Fischer 344 rats (225-250 g, ~10-12 weeks old); Sprague Dawley female rats Dosage: 3 and 10 mg/kg Administration: Oral gavage ; administered BID at 8:00 and 16:00 for 3.5 days Result: Reduced the visceral motor response.Led to a 34-43% inhibition in VMR to colorectal distension (CRD) at 10 mg/kg.

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	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
50 mM	0.043 ml	0.214 ml	0.428 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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RET Kinase inhibitor 1

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

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)