KPT-9274

SKU: orb1226001

Description

KPT-9274 is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120 nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30 nM in MS-751 cell MTT assay; attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines (IC50=600 nM for Caki-1 cells); attenuates G2/M transit and induces apoptosis, shows specificity for attenuation of NAD biosynthesis targets preferentially in RCC cells; decreases tumor growth in xenograft model of RCC.Blood Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 1643913-93-2
• MW: 610.625
• Purity: >98% (HPLC)
• Formula: C₃₅H₂₉F₃N₄O₃
• SMILES: OC(/C=C/C1=NC(N)=CC=C1)=N\CC2=CC3=CC(C4=CC=C(C(N5CCC(F)(F)CC5)=O)C=C4)=CC(C6=CC=C(F)C=C6)=C3O2
• Target: PAK
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  Animal model: Mice. Dosage: 100 mg/kg or 200 mg/kg. Administration: Oral administation; 100 mg/kg or 200 mg/kg; twice a day; 14 days. Result: Showed a significant decrease of xenograft growth in KPT-9274 treated mouse.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KPT9274

Quick Database Links

Gene Symbol

PAK