Elacestrant (hydrochloride)

Elacestrant is a selective estrogen receptor degrader (SERD). It selectively binds to estrogen receptor alpha (ERalpha) over ERbeta (IC50s = 48 and 870 nM, respectively) and reduces ERalpha levels in MCF-7 cells (EC50 = 0.6 nM). Elacestrant reduces MCF-7 proliferation induced by 17beta-estradiol (E2, Cay-10006315) (EC50 = 4 pM). In vivo, elacestrant (30 and 60 mg/kg) reduces E2-induced tumor growth in an MCF-7 mouse xenograft model. It increases survival in an MCF-7 intracranial mouse xenograft model. Elacestrant (0.1-3 mg/kg) protects against bone loss in ovariectomized rats.Formal Name: 6R-[2-[ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-2-naphthalenol, dihydrochloride. CAS Number: 1349723-93-8. Synonyms: RAD901. Molecular Formula: C30H38N2O2 . 2HCl. Formula Weight: 531.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: CCNCCC1=CC=C(CN(C2=CC(OC)=CC=C2[C@H]3CC4=CC=C(O)C=C4CC3)CC)C=C1.Cl.Cl. InChi Code: InChI=1S/C30H38N2O2.2ClH/c1-4-31-17-16-22-6-8-23(9-7-22)21-32(5-2)30-20-28(34-3)14-15-29(30)26-11-10-25-19-27(33)13-12-24(25)18-26,,/h6-9,12-15,19-20,26,31,33H,4-5,10-11,16-18,21H2,1-3H3,2*1H/t26-,,/m1../s1. InChi Key: XGFHYCAZOCBCRQ-FBHGDYMESA-N.