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KPT9274

Name: KPT9274
Brand: TargetMol
SKU: T4354
Price: 56 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4354Cas No. 1643913-93-2

Alias PAK4-IN-1, KPT-9274, KPT 9274

KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

KPT9274

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Purity: 99.93%

Catalog No. T4354Alias PAK4-IN-1, KPT-9274, KPT 9274Cas No. 1643913-93-2

KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$56	In Stock	In Stock
5 mg	$147	In Stock	In Stock
10 mg	$239	In Stock	In Stock
25 mg	$396	In Stock	In Stock
50 mg	$569	In Stock	In Stock
100 mg	$778	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$198	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:99.93%

Color:White

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Product Introduction

Bioactivity

Description	KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.
Targets&IC50	PAK4:100 nM, NAMPT:~120 nM
In vitro	In several human RCC cell lines, KPT-9274 interferences with PAK4 and NAD biosynthetic pathways leading to reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration. The inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc.
In vivo	In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity.
Cell Research	786-0, ACHN, Caki-1 and U-2 OS cells are treated with KPT-9274 (1 μM and 5 μM) incubating for 12 hours.
Animal Research	786-O (VHL-mut) human RCC xenograft model (nude mice) is treated with KPT-9274 (100 and 200 mg/kg),prepared in 58% Polyvinylpyrrolidone K30 + 21% methyl cellulose + 21% Phospholipon 90 g, by oral gavage.
Synonyms	PAK4-IN-1, KPT-9274, KPT 9274

Chemical Properties

Molecular Weight	610.62
Formula	C₃₅H₂₉F₃N₄O₃
Cas No.	1643913-93-2
Smiles	Nc1ccc(\C=C\C(=O)NCc2cc3cc(cc(-c4ccc(F)cc4)c3o2)-c2ccc(cc2)C(=O)N2CCC(F)(F)CC2)cn1
Relative Density.	1.39 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: 55 mg/mL (90.07 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (4.09 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	1.6377 mL	8.1884 mL	16.3768 mL	81.8840 mL
5 mM	0.3275 mL	1.6377 mL	3.2754 mL	16.3768 mL
10 mM	0.1638 mL	0.8188 mL	1.6377 mL	8.1884 mL
20 mM	0.0819 mL	0.4094 mL	0.8188 mL	4.0942 mL
50 mM	0.0328 mL	0.1638 mL	0.3275 mL	1.6377 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