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KPT9274

Catalog No. T4354   CAS 1643913-93-2
Synonyms: KPT-9274, KPT 9274, PAK4-IN-1

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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KPT9274 Chemical Structure
KPT9274, CAS 1643913-93-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 56.00
5 mg In stock $ 147.00
10 mg In stock $ 239.00
25 mg In stock $ 396.00
50 mg In stock $ 569.00
100 mg In stock $ 778.00
1 mL * 10 mM (in DMSO) In stock $ 198.00
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Purity: 99.93%
Purity: 99.73%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 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, KPT 9274, PAK4-IN-1
Molecular Weight 610.62
Formula C35H29F3N4O3
CAS No. 1643913-93-2

Storage

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

Solubility Information

DMSO: 55 mg/mL (90.07 mM)

TargetMolReferences 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:
Drug Repurposing Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Preclinical Compound Library Glycometabolism Compound Library Bioactive Compound Library Orally Active Compound Library

Related Products

Related compounds with same targets
Nampt activator-1 Teglarinad chloride LB-60-OF61 (E)-Daporinad NAMPT degrader-3 OT-82 GNE-617 Nampt-IN-5

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Keywords

KPT9274 1643913-93-2 Cytoskeletal Signaling Metabolism PAK NAMPT KPT-9274 KPT 9274 PAK4-IN-1 inhibitor inhibit

 

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