产品描述:
Alofanib is an allosteric inhibitor of FGFR2.{58160,58161} It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2α) in KATO III gastric carcinoma cells (IC50 = 50s = 370 and 210 nM, respectively). It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) induced by basic FGF (bFGF; IC50 = 11 nM) and tube formation of SVEC4-10 endothelial cells when used at a concentration of 50 nM.{58160} It also inhibits migration of SVEC4-10 cells in a wound healing assay. Alofanib (50 mg/kg) decreases the number of microvessels in tumor tissue by 50% in a SKOV3 ovarian serous carcinoma mouse model. It reduces tumor growth in mouse xenograft models when administered at a dose of 30 mg/kg per day, and the degree of tumor volume reduction positively correlates with the expression level of FGFR2{58161}