R162

GDH1抑制剂(IC50=23µM)；降低人类H1299肺癌和MDA-MB-231乳腺癌细胞内富马酸水平并增加线粒体ROS生成；抑制10-40µM的一组人类癌细胞系增殖但不抑制正常人类细胞；在20mg/kg剂量下降低H1299小鼠异种移植模型中的肿瘤生长和肿瘤内GDH1活性；降低肝激酶B1缺陷型肺癌PDX小鼠模型中的肝转移。A GDH1 inhibitor (IC50 = 23 µM); decreases intracellular fumarate levels and increases mitochondrial ROS production in human H1299 lung and MDA-MB-231 breast cancer cells; inhibits proliferation in a panel of human cancer cell lines but not normal human cells from 10-40 µM; reduces tumor growth and intratumoral GDH1 activity in an H1299 mouse xenograft model at 20 mg/kg; reduces liver metastasis in a liver kinase B1-deficient lung cancer PDX mouse model.分子式C17H12O3分子量264.3O=C1C2=C(C=CC(CC=C)=C2O)C(C3=CC=CC=C31)=O