Description
VLX600 is a compound that shows selective cytotoxicity against quiescent cancer cells (IC
50 = 1-10 μM) with selectivity for malignant cells. It induces necrosis in non-proliferating quiescent core cells in multicellular spheroids (MCs) formed from HCT116 colon cancer cells. VLX600 induces the expression of genes associated with hypoxia, glycolysis, and p53 signaling, stimulates autophagy, and triggers mitochondrial dysfunction in MCs. It displays antitumor activity against colon cancer xenografts with minimal systemic toxicity in mice.
References
zhang x, frykns m, hernlund e, et al. induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments. nat commun. 2014;5:3295.