KPT9274

SKU: orb1302924

Description

KPT9274 (PAK4-IN-1) is an orally active small molecule that non-competitively inhibits both PAK4 and NAMPT with an IC50 of approximately 120 nM. This dual inhibitor is a valuable research tool for studying cancer metabolism and signaling pathways in both cellular and animal models.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1643913-93-2
• MW: 610.62
• Purity: 99.93% (May vary between batches)
• Formula: C₃₅H₂₉F₃N₄O₃
• SMILES: Nc1ccc(\C=C\C(=O)NCc2cc3cc(cc(-c4ccc(F)cc4)c3o2)-c2ccc(cc2)C(=O)N2CCC(F)(F)CC2)cn1
• Target: NAMPT,PAK
• Solubility: DMSO:55 mg/mL (90.07 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (4.09 mM)

Bioactivity

• Target IC50:
  NAMPT:~120 nM|PAK4:100 nM
• In Vivo:
  In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity.
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KPT 9274, KPT9274, KPT-9274, NAMPT, PAK4, PAK4-IN-1

Compound Identifiers

PubChem CID

117779453