CB-6644

SKU: orb1940811

Description

CB-6644 is a selective inhibitor of the RUVBL1/2 complex and blocks the ATPase activity of RUVBL1/2 (IC50 = 15 nM).(In Vitro):CB-6644 (20 μM) interacts with the RUVBL1/2 complex in Ramos cells. In 123 cell lines such as HCT116, NCI-1975, and HT29 cells, CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines (EC50: 41 to 785 nM).(In Vivo):Administration of oral gavage once (qd) or twice (BID) daily, 10 days of treatment for Ramos, 30 days of treatment for RPMI8226, CB-6644 has antitumor activity in xenograft tumor models. The tumor growth inhibitions (TGIs) are 68 and 81%, respectively in Ramos xenograft models and RPMI8226 xenograft models.

Key Properties

• CAS Number: 2316817-88-4
• MW: 573.06
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₄ClFN₄O₅
• SMILES: CCOc1cc(F)c(Cl)cc1C(=O)NCC(C)(C)CC(=O)Nc1c(COC)n2CCCc3ccccc3-n2c1=O
• Solubility: In Vitro: DMSO : 100 mg/mL (174.50 mM)

Bioactivity

• In Vivo:
  Animal model: SCID-beige mice bearing human tumor xenografts derived from either Burkitt’s lymphoma (Ramos) or multiple myeloma (RPMI8226) cell lines. Dosage: 150 mg/kg. Administration: Oral gavage once (qd) or twice (BID) daily, 10 days of treatment for Ramos, 30 days of treatment for RPMI8226. Result: There was no significant bodyweight loss in mice. TGI of 68 and 81% in Ramos and RPMI8226, respectively.
• In Vitro:
  Cell Viability Assay Cell line: 123 cell lines such as HCT116, NCI-1975, and HT29 cells. Concentration: 0.001, 0.01, 0.1, 1, and 10 μM Incubation time: 72 hours. Result: Potently killed cells with an EC50 range of 41 to 785 nM.

Storage & Handling

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