Compound 13 Methuosis inducer RGNCY-0082
Per 10 mg
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 .
Huang W et al. Discovery and Identification of Small Molecules as Methuosis Inducers with In Vivo Antitumor Activities. J. Med. Chem., Just Accepted Manuscript. DOI:10.1021/acs.jmedchem.8b00753. Publication Date (Web): 07 Jun 2018.
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