CB-6644 (C007B-343197)

CB-6644 is a selective inhibitor of RUVBL1 / 2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC 50 of 15 nM.In VitroCB-6644 (20 µM) interacts with the RUVBL1/2 complex in Ramos cells. CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines (including HCT116, NCI-1975, and HT29 cells) with an EC 50 range of 41 to 785 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 EC 50 range of 41 to 785 nM.In VivoCB-6644 (150 mg/kg, oral administration, 10 days of treatment for SCID-beige mice bearing Ramos xenograft models, 30 days of treatment for SCID-beige mice bearing RPMI8226 xenograft models) has antitumor activity in xenograft tumor models with tumor growth inhibitions (TGIs) of 68 and 81%, respectively in Ramos xenograft models and RPMI8226 xenograft models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:Solid. Specification: 0.99 Molecular Formula: C29H34ClFN4O5 Molecular Weight: 573.06 PubChem CID: 137333455 Isomeric SMILES: CCOC1=CC(=C(C=C1C(=O)NCC(C)(C)CC(=O)NC2=C(N3CCCC4=CC=CC=C4N3C2=O)COC)Cl)F