纯度:>97% by HPLC: Agilent Poroshell 120 C18, 80/20 MeOH/water, 0.8 mL/min, 245 and 270 nm.;NMR (Conforms)
分子式:C26H24F3N7O3S
分子量:571.57
溶剂:DMSO
性状:Pale yellow solid
存储:-20°C
Activity (short version):Glutaminase inhibitor
Function / Pharmacology:CB-839 is a potent (IC50 = 24 nM), selective and orally bioavailable inhibitor of glutaminase (KGA and GAC).1 CB-839 displayed an antiproliferative effect in the triple-negative breast cancer cell line, HCC-1806, but no activity in the estrogen receptor-positive cell line T47D. CB-839 was able to cause proliferation arrest and apoptosis in acute myeloid leukemia cells without causing cytotoxicity against normal human CD34(+) progenitors.2 Aspartate-glutamate carrier 1 (AGC1) inhibition can synergize with CB-839 to limit tumor growth.3