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KPT9274

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Purity:99.93%

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COA HNMR HPLC

KPT9274

Catalog No. T4354Cas 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.

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Pack Size	Price	Availability
1 mg	$56	In Stock
5 mg	$147	In Stock
10 mg	$239	In Stock
25 mg	$396	In Stock
50 mg	$569	In Stock
100 mg	$778	In Stock
1 mL x 10 mM (in DMSO)	$198	In Stock

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

Chemical Properties

Molecular Weight	610.62
Formula	C35H29F3N4O3
Cas No.	1643913-93-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (90.07 mM)

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 mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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