ARN810

ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERalpha and ERbeta (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERalpha in MCF-7 cells (EC50 = 0.7 nM). It inhibits ERalpha transcriptional activity induced by 17beta-estradiol (Cay-10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17beta-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.Formal Name: (2E)-3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-2-propenoic acid. CAS Number: 1365888-06-7. Synonyms: GDC-0810, RG-6046. Molecular Formula: C26H20ClFN2O2. Formula Weight: 446.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10mg/mL, DMSO: 15mg/mL, Ethanol: 20mg/mL, Ethanol:PBS (pH 7.2) (1:4): 0.2mg/mL. SMILES: ClC1=C(/C(CC)=C(C2=CC=C(/C=C/C(O)=O)C=C2)/C3=CC(C=NN4)=C4C=C3)C=CC(F)=C1. InChi Code: InChI=1S/C26H20ClFN2O2/c1-2-21(22-10-9-20(28)14-23(22)27)26(18-8-11-24-19(13-18)15-29-30-24)17-6-3-16(4-7-17)5-12-25(31)32/h3-15H,2H2,1H3,(H,29,30)(H,31,32)/b12-5+,26-21+. InChi Key: BURHGPHDEVGCEZ-KJGLQBJMSA-N.