产品描述:
Palomid 529 (P529) is an inhibitor of mammalian target of rapamycin complex (mTORC) formation.{39092} It is a derivative of a non-steroidal estrogen antagonist that has anti-angiogenic and anticancer activity but lacks estrogen receptor binding activity in estrogen binding assays in vitro. Palomid 529 inhibits VEGF-driven and bFGF-driven endothelial cell proliferation (IC50s = 20 and 30 nM, respectively) and reduces VEGF-A-driven phosphorylation of AktS473, an mTORC2 substrate. In vivo, palomid 529 inhibits retinal neovascularization in mice with oxygen-induced retinopathy, a commonly used assay for pathogenic angiogenesis, Ad-VEGF-A-driven angiogenesis, and phosphorylation of AktS473. Palomid 529 has anticancer effects in glioma cancer cells and xenografts via AktS473 signaling downtstream of mTORC.