BAY-876 |
Katalog-Nr.GC19061 |
BAY-876 ist ein oral aktiver und selektiver Glucosetransporter 1 (GLUT1)-Inhibitor mit einem IC50 von 2 nM. BAY-876 ist >130-mal selektiver fÜr GLUT1 als GLUT2, GLUT3 und GLUT4. BAY-876 ist auch ein starker Blocker des glykolytischen Metabolismus und des Wachstums von Eierstockkrebs.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1799753-84-6
Sample solution is provided at 25 µL, 10mM.
BAY-876 is a selective glucose transporter 1 (GLUT1) inhibitor with IC50 of 2 nM[1]. The IC50 of BAY-876 for GLUT2, GLUT3 and GLUT4 are 10.8, 1.67 and 0.29μM, respectively[1]. BAY-876 blocks glucose transport into tumor cells by inhibiting GLUT activity, thereby effectively inhibiting glucose uptake and tumor cell growth [2].
In vitro, BAY-876 (75nM) treated SKOV-3, OVCAR-3, HEY and A2780 cells for 72h and had a growth inhibitory effect on SKOV-3, OVCAR-3 and HEY cells, but not on A2780 cells [3] . BAY-876 (10 nM, 25 nM, 50 nM) treated CD4+ T cells and macrophages for 24 hours, significantly weakening the glucose uptake of cells and reducing the levels of inflammatory factors [4]. BAY-876 (10-1000µM) treated the renal adenocarcinoma 786-O cell line for 96 hours and significantly inhibited cell proliferation, with an IC50 of 53.56µM [5].
In vivo, BAY-876 (0, 1.5, 3.0, and 4.5 mg/kg/day) dose-dependently reduced tumor volume in NSG mice harboring SKOV-3 xenografts administered orally for 4 weeks and was effective in mice. Body weight has no effect [3]. BAY-876 (5 mg/kg/day) was administered orally for 2 days to mice bearing MHCC 97-H xenografts, which significantly inhibited tumor tissue formation and glucose uptake by cells in the tissue [6].
References:
[1] Siebeneicher H, Cleve A, Rehwinkel H, et al. Identification and optimization of the first highly selective GLUT1 inhibitor BAY‐876[J]. ChemMedChem, 2016, 11(20): 2261-2271.
[2] Kopitz C, Toschi L, Algire C, et al. Pharmacological characterization of BAY-876, a novel highly selective inhibitor of glucose transporter (GLUT)-1 in vitro and in vivo[J]. Cancer Research, 2016, 76(14_Supplement): 4746-4746.
[3] Ma Y, Wang W, Idowu M O, et al. Ovarian cancer relies on glucose transporter 1 to fuel glycolysis and growth: anti-tumor activity of BAY-876[J]. Cancers, 2018, 11(1): 33.
[4] Chen Z, Vaeth M, Eckstein M, et al. Characterization of the effect of the GLUT-1 inhibitor BAY-876 on T cells and macrophages[J]. European Journal of Pharmacology, 2023, 945: 175552.
[5] Peshraw Salih Hamadamin, et al. Exploring the anticancer potential of hydrogen sulfide and BAY876 on clear cell renal cell carcinoma cells: Uncovering novel mutations in VHL and KDR genes among ccRCC patients[J]. Molecular and Clinical Oncology, 2024.
[6] Yang H, Zhang M Z, Sun H, et al. A novel microcrystalline BAY-876 formulation achieves long-acting antitumor activity against aerobic glycolysis and proliferation of hepatocellular carcinoma[J]. Frontiers in Oncology, 2021, 11: 783194.
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