RGNCY-0082 (Compound 13 Methuosis inducer)
Methuosis is a novel non-apoptotic mechanism of cell death that is characterized by cytoplasmic vacuole accumulation. Compound 13 is a novel potent vacuole-inducer and displayed differential toxicities across a broad range of cancer cell lines (including MCF-7, MDA-MB-231, HCT116 and A375) but had no effect on the non-tumorigenc epithelial cell line, MCF-10A. Compound 13 was demonstrated to cause cell death via methuosis. Compound 13 did not demonstrate any side effects despite significant pharmacological efficacy in the suppression of MDA-MB-231 tumor growth in a xenograft mouse model. Compound 13 is the first methuosis inducer with efficacy in vivo and shows therapeutic potential in targeting methuosis in cancer treatment. A375 IC50 = 0.326+0.026µM , MDA-MB-231 IC50 = 1.571+0.066µM , MCF7 IC50 = 2.611+0.739µM , HCT116 IC50 = 1.008+0.042µM .
Tags: Cancer, small molecule, breast cancer, MCF-7, MDA-MB-231, MCF-10A, RGNCY-0082, Compound 13, methuosis, HCT116, A375