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NSC781406

Name: NSC781406
Brand: TargetMol
SKU: T16355
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16355Cas No. 1676893-24-5

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

NSC781406

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Purity: 99.58%

Catalog No. T16355Cas No. 1676893-24-5

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$58	In Stock	In Stock
10 mg	$94	In Stock	In Stock
25 mg	$171	In Stock	In Stock
50 mg	$257	In Stock	In Stock
100 mg	$395	In Stock	In Stock
200 mg	$562	-	In Stock
1 mL x 10 mM (in DMSO)	$81	In Stock	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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Purity:99.58%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).
Targets&IC50	PI3Kβ:9.4 nM, PI3Kα:2 nM, mTOR:5.4 nM, PI3Kδ:14 nM, PI3Kγ:2.7 nM
In vitro	NSC781406 shows reasonable liver microsome stability. NSC781406 displays effective PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM) and it also demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is effective against 60 cancer cell lines with a mean GI50 value of 65 nM and with a GI50 value of less than 10 nM against four cancer cell lines.
In vivo	NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight. NSC781406(30 mg/kg) treatment, causes statistically significant antitumor activity, in the xenograft models. It has a mean reduction in the relative tumor volume ratio of 52%. Sorafenib shows an inhibition ratio of 44% at 50 mg/kg .

Chemical Properties

Molecular Weight	627.68
Formula	C₂₉H₂₇F₂N₅O₅S₂
Cas No.	1676893-24-5
Smiles	COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(C#CCN3CCN(CC3)S(C)(=O)=O)c2c1
Relative Density.	1.52 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: 150 mg/mL (238.98 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 4 mg/mL (6.37 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	1.5932 mL	7.9658 mL	15.9317 mL	79.6584 mL
5 mM	0.3186 mL	1.5932 mL	3.1863 mL	15.9317 mL
10 mM	0.1593 mL	0.7966 mL	1.5932 mL	7.9658 mL
20 mM	0.0797 mL	0.3983 mL	0.7966 mL	3.9829 mL
50 mM	0.0319 mL	0.1593 mL	0.3186 mL	1.5932 mL
100 mM	0.0159 mL	0.0797 mL	0.1593 mL	0.7966 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