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GSK251

Name: GSK251
Brand: TargetMol
SKU: T39573
Price: 166 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39573Cas No. 2125968-05-8

GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.

GSK251

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Purity: 99.8%

Catalog No. T39573Cas No. 2125968-05-8

GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$166	-	In Stock
5 mg	$417	-	In Stock
10 mg	$592	-	In Stock
25 mg	$882	-	In Stock
50 mg	$1,180	-	In Stock
100 mg	$1,600	-	In Stock

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

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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Batch Information

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Purity:99.8%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

GSK251 AI Summary

GSK251 shows potent inhibitory activity against the PI3K isoforms PI3Kalpha, PI3Kbeta, PI3Kdelta, and PI3Kgamma PH domains, with an IC50 value of <= 10000.0 nM when tested using a TR-FRET assay. Notably, it exhibits high affinity and selectivity for PI3Kdelta, demonstrating low nanomolar IC50 and Ki values of 0.7943 nM and 0.01259 nM, respectively. The compound also has good oral bioavailability (46.0%) and moderate clearance in rats, with a half-life of 2.6 hours, indicating its potential as an effective PI3K inhibitor with promising pharmacokinetic properties..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.

Chemical Properties

Molecular Weight	584.71
Formula	C₂₉H₃₇FN₆O₄S
Cas No.	2125968-05-8
Smiles	COc1ncc(cc1S(=O)(=O)Nc1ccnc(c1)-c1ccc(CN2CCN(CC2)C(C)C)cc1F)N1CCOCC1
Relative Density.	1.295 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

DMSO: 50 mg/mL (85.51 mM), Sonication and heating to 60℃ are recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.42 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7102 mL	8.5512 mL	17.1025 mL	85.5125 mL
5 mM	0.3420 mL	1.7102 mL	3.4205 mL	17.1025 mL
10 mM	0.1710 mL	0.8551 mL	1.7102 mL	8.5512 mL
20 mM	0.0855 mL	0.4276 mL	0.8551 mL	4.2756 mL
50 mM	0.0342 mL	0.1710 mL	0.3420 mL	1.7102 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