BAY-876

BAY-876 is a potent and highly selective small molecule inhibitor of glucose transporter type 1 (GLUT1), with an IC50 of approximately 2 nM for GLUT1 and significantly lower activity against other glucose transporters such as GLUT2, GLUT3, and GLUT4[1][3]. It is cell-permeable and orally bioavailable. By inhibiting GLUT1-mediated glucose uptake, BAY-876 disrupts glycolytic metabolism in cancer cells—a process often upregulated in tumors (the Warburg effect)—leading to reduced ATP production and inhibition of cell proliferation[6][8]. Preclinical studies have demonstrated its anti-tumor activity in various cancer models including colorectal cancer, ovarian cancer, hepatocellular carcinoma (HCC), and bladder cancer[2][5][6]. The drug has also been formulated as a microcrystalline injectable for localized delivery in HCC models to achieve sustained antitumor effects with limited systemic exposure[2]. Initially developed by Bayer AG as an experimental research tool compound targeting metabolic vulnerabilities in cancers overexpressing GLUT1[5].

Other names

N4-(1-(4-Cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-7-fluoroquinoline-2,4-dicarboxamide