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GSK2983559 active metabolite

Name: GSK2983559 active metabolite
Brand: TargetMol
SKU: T5401
Price: 412 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.57%

货号 T5401Cas号 1423186-80-4

GSK2983559 active metabolite (RIPK2-IN-1) 是一种受体相互作用蛋白-2 激酶抑制剂。

GSK2983559 active metabolite

一键复制产品信息

很棒

纯度: 99.57%

货号 T5401Cas号 1423186-80-4

GSK2983559 active metabolite (RIPK2-IN-1) 是一种受体相互作用蛋白-2 激酶抑制剂。

规格	价格	库存
1 mg	¥ 412	现货
5 mg	¥ 993	现货
10 mg	¥ 1,570	现货
25 mg	¥ 2,860	现货
50 mg	¥ 4,120	现货
100 mg	¥ 5,880	现货
200 mg	¥ 7,920	现货
1 mL x 10 mM (in DMSO)	¥ 982	现货

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实验操作小课堂

常见问题解答

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纯度: 99.57%

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资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

GSK2983559 active metabolite AI Summary

GSK2983559 active metabolite exhibits significant bioactivity across several assays. It effectively inhibits multiple kinases, including STK10, VEGFR2, EPHA6, ABL2, and VEGFR3 at a concentration of 1 μM. The compound also shows inhibition of ERG, RIP2K, NOD2, and RIPK2 with IC50 values ranging from 2.0 nM to 26.0 nM, and of TLR9 and TLR2 with IC50 values greater than 10000.0 nM. Additionally, GSK2983559 active metabolite has high oral bioavailability in various animal models (Sprague-Dawley rat, Beagle dog, Gottingen minipig), displaying varied clearance rates and volumes of distribution. It demonstrates anti-inflammatory activity in patient-derived inflamed intestinal mucosa of Crohn's disease and ulcerative colitis and passive permeability in MDCK cells. In cancer-related assays, GSK2983559 active metabolite shows antiproliferative activity against human UCH1 cells (IC50 > 50000.0 nM) and UCH2 cells (IC50 of 30000.0 nM) after 72 hours, as measured by alamar blue assay. It inhibits EGFR in human A431 cells with an IC50 greater than 50000.0 nM, assessed by reduction in EGF-stimulated EGFR autophosphorylation after 90 minutes of preincubation. Additionally, the compound inhibits tracer 5 binding to human N-terminal nano luciferase-fused GAK in HEK293 cells at 5 μM with an inhibition rate of 0.0% after 2 hours by nanoBRET assay. In terms of cytotoxicity, it has an IC50 greater than 50000.0 nM against human WS1 cells, indicating low cytotoxicity. Furthermore, GSK2983559 active metabolite shows moderate binding affinity to C-terminal AVI-tagged GAK expressed in Escherichia coli and demonstrates strong target engagement by displacing fluorescent tracers from the N-terminus of human GAK and human RIPK2. Notably, the compound is not highly cytotoxic against human LNCAP and 22Rv1 cells based on MTS assay results..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

化学信息

分子量	458.55
分子式	C₂₁H₂₂N₄O₄S₂
CAS No.	1423186-80-4
Smiles	CC(C)(C)S(=O)(=O)c1cc2c(Nc3ccc4scnc4c3)ncnc2cc1OCCO
密度	1.423 g/cm3 (Predicted)

储存&溶解度

存储

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 32 mg/mL (69.79 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 2 mg/mL (4.36 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1808 mL	10.9039 mL	21.8079 mL	109.0394 mL
5 mM	0.4362 mL	2.1808 mL	4.3616 mL	21.8079 mL
10 mM	0.2181 mL	1.0904 mL	2.1808 mL	10.9039 mL
20 mM	0.1090 mL	0.5452 mL	1.0904 mL	5.4520 mL
50 mM	0.0436 mL	0.2181 mL	0.4362 mL	2.1808 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法： 取 100 μL DMSO 母液，添加 400 μL PEG300 混匀澄清，再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH₂O 混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300， PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

关键词

RIPkinase RIP2 RIP kinase GSK-2983559 active metabolite GSK2983559 active metabolite GSK-2983559 GSK 2983559

GSK2983559 active metabolite

GSK2983559 active metabolite