Palazestrant

An ERalpha antagonist (IC50 = 6.4 nM), induces degradation of ERalpha in MCF-7 cells (EC50 = 0.52 nM), decreases the proliferation of MCF-7 and CAMA-1 breast cancer cells (IC50s = 1.8 and 1.7 nM, respectively), inhibits estradiol-induced cell cycle progression in the same cells at 100 nM, reduces tumor growth and increases survival alone and in combination with ribociclib in an estradiol-stimulated PDX mouse model of breast cancer at 10 mg/kg per day. Formulation: A solid. InChI: InChI=1S/C28H36FN3O/c1-5-14-31-16-22(17-31)33-21-12-10-20(11-13-21)27-26-24(23-8-6-7-9-25(23)30-26)15-19(2)32(27)18-28(3,4)29/h6-13,19,22,27,30H,5,14-18H2,1-4H3/t19-,27-/m1/s1. InChIKey: LBSFUBLFDCAEKV-XHCCPWGMSA-N. SMILES: C[C@H](CC1=C2NC3=CC=CC=C31)N(CC(F)(C)C)[C@@H]2C4=CC=C(OC5CN(CCC)C5)C=C4