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GNE-490

Name: GNE-490
Brand: TargetMol
SKU: T22339
Price: 77 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22339Cas No. 1033739-92-2

GNE-490 is an effective inhibitor of pan-PI3K with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50 = 750 nM).

GNE-490

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Purity: 99.77%

Catalog No. T22339Cas No. 1033739-92-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$77	-	In Stock
2 mg	$117	-	In Stock
5 mg	$198	-	In Stock
10 mg	$338	-	In Stock
25 mg	$535	-	In Stock
50 mg	$738	-	In Stock
100 mg	$980	-	In Stock
200 mg	$1,350	-	In Stock
1 mL x 10 mM (in DMSO)	$215	-	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:99.77%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

GNE-490 AI Summary

GNE-490 exhibits multiple bioactivities including antiproliferative activity against human PC3 cells deficient in PTEN and MCF7.1 cells expressing PI3Kalpha mutant. It inhibits various kinases such as PI3K isoforms (alpha, beta, gamma, delta), mTOR, and PIK3C2beta. Additionally, it significantly inhibits the PI3K/Akt/mTOR pathway signaling in PI3Kalpha mutant expressing human MCF7.1 cells xenografted in nu/nu mice, indicated by decreased phosphorylation of Akt, Pras40, and S6RP. GNE-490 shows high oral bioavailability and moderate to high protein binding in mouse plasma. It has favorable pharmacokinetic parameters, including clearance, volume of distribution, area under the curve, and half-life. Furthermore, it demonstrates strong antitumor activity, resulting in tumor growth inhibition in human MCF7.1 cells expressing PI3Kalpha mutant xenografted in nu/nu mice..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	GNE-490 is an effective inhibitor of pan-PI3K with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50 = 750 nM).
Targets&IC50	PI3Kδ:5.2 nM, PI3Kβ:25 nM, PI3Kγ:15 nM, mTOR:750 nM, PI3Kα:3.5 nM

Chemical Properties

Molecular Weight	386.47
Formula	C₁₈H₂₂N₆O₂S
Cas No.	1033739-92-2
Smiles	Cc1nc(N)ncc1-c1nc(N2CCOCC2)c2sc(cc2n1)C(C)(C)O
Relative Density.	no data available

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 (129.38 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5875 mL	12.9376 mL	25.8752 mL	129.3761 mL
5 mM	0.5175 mL	2.5875 mL	5.1750 mL	25.8752 mL
10 mM	0.2588 mL	1.2938 mL	2.5875 mL	12.9376 mL
20 mM	0.1294 mL	0.6469 mL	1.2938 mL	6.4688 mL
50 mM	0.0518 mL	0.2588 mL	0.5175 mL	2.5875 mL
100 mM	0.0259 mL	0.1294 mL	0.2588 mL	1.2938 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