GSK3179106|cas:1627856-64-7|西域试剂

GSK3179106,98.41%

产品编号：Bellancom-100459| CAS NO：1627856-64-7| 分子式：C₂₂H₂₁F₄N₃O₄| 分子量：467.41

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100459	￥500.00	杭州北京（现货）
Bellancom-100459	￥1100.00	杭州北京（现货）
Bellancom-100459	￥2000.00	杭州北京（现货）
Bellancom-100459	￥8000.00	杭州北京（现货）
Bellancom-100459	￥14500.00	杭州北京（现货）

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GSK3179106

产品介绍

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 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.

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.

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

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
(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.

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

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.

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.

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

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.

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.

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (213.94 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1394 mL	10.6972 mL	21.3945 mL
5 mM	0.4279 mL	2.1394 mL	4.2789 mL
10 mM	0.2139 mL	1.0697 mL	2.1394 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。