CB-5339

SKU: orb2900886

Description

CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research. CB-5339 extracted from WO2015109285A1 compound FF07.

Key Properties

• CAS Number: 1863952-15-1
• MW: 412.49
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₄N₆O
• SMILES: CC=1N(C=2C(=C(C(N)=O)C=CC2)C1)C3=NC(NCC4=CC=CC=C4)=C5C(N3)=NCCC5
• Solubility: In Vitro: DMSO : 100 mg/mL (242.43 mM; Ultrasonic (<80°C)

Bioactivity

• In Vivo:
  Animal model: MLL-AF9-driven patient-derived xenograft (PDX) AML model in C57BL/6 male mice. Dosage: 90 mg/kg. Administration: oral gavage (p.o.). Result: Decreased bone marrow leukemic infiltration and circulating leukemic cells.
• In Vitro:
  Western blot analysis. Cell line: MV4-11 AML cell line. Concentration: 0, 0.2, 0.4, 0.8, 1.6 μM Incubation time: 24-48 hours. Result: Induced dose-dependent polyubiquitin protein accumulation at concentrations ≥ 0.4 μM. Induced the ER stress marker GRP78 accumulated at concentrations ≥ 0.4 μM. Induced spliced XBP-1 and ATF-4 accumulated after treatment with CB-5339 at concentrations ≥ 1.6 μM and 0.8 μM respectively arguing for a concentration-dependent increase in proteotoxic stress.

Storage & Handling

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