谷氨酰胺酶抑制剂;Glutaminase Inhibitors;;InformationUPGL00004 UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.Targetsglutaminase C (Cell-free assay) 29 nMIn vitroUPGL00004 potently inhibits the growth of triple negative breast cancer cells, as well as tumor growth when combined with the anti-VEGF antibody bevacizumab.In vivoUPGL00004 potently suppresses tumor growth in a patient-derived xenograft model for breast cancer, when combined with the anti-angiogenesis, anti-VEGF monoclonal antibody bevacizumab.Cell Research(from reference)Cell lines:Breast cancer cells Concentrations:0-10 μM Incubation Time:6 days
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IC50: 29 nM (Glutaminase C);Kd: 27 nM (Glutaminase C)