产品描述:
ERD-308 is a proteolysis-targeting chimera (PROTAC) containing the selective estrogen receptor modulator raloxifene (Item No. 10011620) conjugated to VHL ligand 1 (Item No. 21591).{67761} It induces degradation of estrogen receptor α (ERα) in MCF-7 and T47D breast cancer cells with half-maximal degradation concentration (DC50) values of 0.17 and 0.43 nM, respectively. ERD-308 inhibits the growth of MCF-7 cells (GI50 = 0.77 nM). It reduces the levels of mRNA encoding progesterone receptor and gene regulated in breast cancer 1 (GREB1) to an equivalent extent as the selective estrogen receptor degrader fulvestrant (Item No. 10011269) in MCF-7 cells when used at concentrations ranging from 1 to 300 nM.