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GSK2850163

Name: GSK2850163
Brand: TargetMol
SKU: T11488
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11488Cas No. 2121989-91-9

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

GSK2850163

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Purity: 99.04%

Catalog No. T11488Cas No. 2121989-91-9

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$64	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$239	In Stock	In Stock
50 mg	$378	-	In Stock
100 mg	$568	-	In Stock
1 mL x 10 mM (in DMSO)	$70	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.04%

Appearance:Viscous

Color:Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
Targets&IC50	IRE1α kinase activity:20 nM , IRE1α RNase activity:200 nM
In vitro	The increased autophosphorylation of IRE1α could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM).

Chemical Properties

Molecular Weight	446.41
Formula	C₂₄H₂₉Cl₂N₃O
Cas No.	2121989-91-9
Smiles	Cc1ccc(CNC(=O)N2CCC[C@]3(CCN(Cc4ccc(Cl)c(Cl)c4)C3)C2)cc1
Relative Density.	1.28 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 50 mg/mL (112 mM), Sonication is recommended.

DMSO: 150 mg/mL (336.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2401 mL	11.2005 mL	22.4009 mL	112.0047 mL
5 mM	0.4480 mL	2.2401 mL	4.4802 mL	22.4009 mL
10 mM	0.2240 mL	1.1200 mL	2.2401 mL	11.2005 mL
20 mM	0.1120 mL	0.5600 mL	1.1200 mL	5.6002 mL
50 mM	0.0448 mL	0.2240 mL	0.4480 mL	2.2401 mL
100 mM	0.0224 mL	0.1120 mL	0.2240 mL	1.1200 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc