| 产品描述: | VEGFR2 选择性抑制剂;VEGFR2 Selective Inhibitors;;InformationBFH772 is a novel potent oralVEGFR2inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.TargetsVEGFR2 (Cell-free assay) 3 nMIn vitroBFH772 was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.In vivoBFH772 all at 3 mg/kg orally dosed once per day potently inhibited melanoma growth (by 54−90% for primary tumor and 71−96% for metastasis growth).Cell Research(from reference)Cell lines:HUVEC endothelial cells Concentrations:0-10 nM Incubation Time:48 h |