GSK3179106|1627856-64-7|-陌孚医药/Medlife

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GSK3179106

目录号: PL10972 纯度: ≥99%

CAS No. :1627856-64-7

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中文名称	GSK3179106
英文名称	GSK3179106
英文别名	RET Kinase inhibitor 1;GSK3179106;DY8BBK4G3C;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;RET Kinase inhibitor 1?;BCP23560;s8821;ZB1508;2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]acetamide;4-(4-Ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro
Cas No.	1627856-64-7
分子式	C₂₂H₂₁F₄N₃O₄
分子量	467.41
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

GSK3179106 是一种具有口服活性的，选择性的 RET 激酶抑制剂，对人和大鼠 RET 的 IC₅₀ 分别为 0.4 nM 和 0.2 nM。GSK3179106 通过减轻炎症后和应激引起的内脏超敏反应而具有用于肠易激综合征 (IBS) 的潜力。

生物活性

GSK3179106 is an orally active and selective RET kinase inhibitor with IC 50 s 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.

性状

Solid

IC50 & Target[1][2]

IC50: 0.4 nM (human RET), 0.2 nM (rat RET)

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (213.94 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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