MCF7 cells engineered to express one of the most common and aggressive ERα mutations, Y537S...Mice were treated with 3 and 10 mg/kg of OP-1250 alone or in combination with palbociclib at 70mg/kg and tumor growth was monitored...Our results also suggest that the efficacy seen in the combination study was driven primarily by OP-1250. In total, these results demonstrate the potential use of OP-1250, both alone and in combination with a CDK4/6 inhibitor, to inhibit tumor growth and metastasis in a model of aggressive mutant ER+ MBC.