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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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
KPT9274 Chemical Structure
KPT9274, CAS 1643913-93-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 75.00
2 mg In stock $ 108.00
5 mg In stock $ 182.00
10 mg In stock $ 291.00
25 mg In stock $ 582.00
50 mg In stock $ 833.00
100 mg In stock $ 1,150.00
1 mL * 10 mM (in DMSO) In stock $ 246.00
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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:
Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compound Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets
Teglarinad chloride Nampt activator-1 NAMPT degrader-3 OT-82 STF-118804 GNE-618 GNE-617 SBI-797812

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Keywords

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

 

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