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KPT9274

Catalog No. T4354 CAS 1643913-93-2

Synonyms: KPT-9274, PAK4-IN-1, KPT 9274

KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

KPT9274, CAS 1643913-93-2

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Purity: 98%

Biological Description

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Description	KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.
Targets&IC50	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	KPT-9274, PAK4-IN-1, KPT 9274
Molecular Weight	610.637
Formula	C35H29F3N4O3
CAS No.	1643913-93-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Abu Aboud O,etal.Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth.Mol Cancer Ther. 2016 Sep;15(9):2119-29.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library

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Related compounds with same targets

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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.

Keywords

KPT9274 1643913-93-2 代谢细胞骨架 PAK NAMPT KPT 9274 PAK4-IN-1 KPT-9274 Inhibitor inhibitor inhibit

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