1611446-66-2

CAY10726 is an arylurea fatty acid.¹ It decreases ATP production by 28% in MDA-MB-231 breast cancer cells when used at a concentration of 10 μM. CAY10726 decreases proliferation and initiates apoptosis in MDA-MB-231 cells via depletion of the phospholipid cardiolipin and its precursor phosphatidylglycerol from the mitochondrial membrane. In vivo, CAY10726 (2.5-40 mg/kg) reduces tumor volume and increases tumor cell apoptosis in a mouse MDA-MB-231 breast cancer xenograft model in a dose-dependent manner.

Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models[1].

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1. Rawling, T., Choucair, H., Koolaji, N., et al. A novel arylurea fatty acid that targets the mitochondrion and depletes cardiolipin to promote killing of breast cancer cells J. Med. Chem. 60(20),8661-8666(2017).