产品描述:
Vandetanib is a multi-kinase inhibitor that inhibits VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRβ, Tie-2, and FGFR1 in cell-free assays (IC50s = 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively).{53195,24156} It also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM). Vandetanib (1 and 2.5 µM) induces apoptosis and cell cycle arrest at the G0/G1 phase in GEO colon and OVCAR-3 ovarian cancer cells.{53196} It inhibits proliferation of HAK1-B, KYN-2, and Huh7 hepatocarcinoma cells, as well as human umbilical vein endothelial cells (HUVECs), with IC50 values of 10, 8.1, 9.4, and 7.1 µM, respectively.{53197} Vandetanib (200 mg/kg) increases survival and decreases tumor angiogenesis and VEGFR2 levels in a D54MG glioblastoma mouse xenograft model.{53198} It reduces tumor growth in a variety of mouse xenograft models, including lung, colon, and breast cancer models, when administered at doses of 25, 50, and 100 mg/kg per day.{53195} Formulations containing vandetanib have been used in the treatment of medullary thyroid cancer.