产品描述:
GN44028 is an inhibitor of HIF-1α transcriptional activity.{51474} It reduces HIF-1α reporter gene expression in HeLa cervical cancer cells (IC50 = 14 nM). GN44028 induces cytotoxicity in HCT116 colorectal, HepG2 hepatic, PC3 prostate, and HeLa cancer cells (IC50s = 2.1, 3.7, 25.4, and 2.1 µM, respectively). It reduces the levels of VEGF, but not HIF-1α or HIF-1α-HIF-1β dimer levels, in HeLa cells when used at concentrations of 0.1 and 1 µM. In vivo, GN44028 (5 mg/kg twice per week), alone or in combination with 5-fluorouracil (Item. No. 14416), decreases tumor volume and the number of lung metastases and increases survival percentage in a CT26 murine colon cancer model.{51475}