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 IC50 of 15 nM[1].
CB-6644 (20 µM) interacts with the RUVBL1/2 complex in Ramos cells[1]. CB-6644 (0.4 µM, 80 hours) dramatically inhibits HCT116 cells growth rate and robustly induces apoptosis. Z-VAD-FMK alone does not influence the growth or viability of the cells. However, blockade of caspase activity by Z-VAD-FMK results in a partial recovery of the growth of cells treated with CB-6644[1].|| Cell Viability Assay[1]||Cell Line:|HCT116 cells|Concentration:|0.4 µM|Incubation Time:|80 hours|Result:|Inhibited dramatically cell growth rate.
CB-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[1].|| Animal Model:|SCID-beige mice bearing human tumor xenografts derived from either Burkitt's lymphoma (Ramos) or multiple myeloma (RPMI8226) cell lines[1]|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.
[1]. Assimon VA, et al. CB-6644 Is a Selective Inhibitor of the RUVBL1/2 Complex with Anticancer Activity. ACS Chem Biol. 2019 Feb 15;14(2):236-244.