EPI-001

EPI-001 is an androgen receptor antagonist with an IC50 value of approximately 6 µM for inhibition of transactivation of the androgen receptor N-terminal domain (NTD). It inhibits androgen-, FSK-, and IL-6-induced, as well as ligand-independent, prostate-specific antigen (PSA) reporter gene expression in LNCaP cells expressing either the full length androgen receptor or a constitutively active mutant that lacks the ligand binding domain in a dose-dependent manner. EPI-001 inhibits androgen receptor interaction with the PSA androgen response element and blocks androgen-stimulated induction of endogenous PSA and 17 other androgen regulated genes in LNCaP cells. It inhibits androgen-dependent and -independent growth of LNCaP and MDA-PCa-2B cells, but not 22Rv1, DU145, or PC3 cells that do not express the androgen receptor. EPI-001 (50 mg/kg) reduces serum PSA and tumor growth in an LNCaP prostate cancer xenograft model in castrated mice. It also reduces serum PSA in a patient-derived LT313 prostate cancer mouse xenograft model. Formulations containing EPI-001 are under clinical investigation for the treatment of castration-resistant prostate cancer.Formal Name: 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol. CAS Number: 227947-06-0. Molecular Formula: C21H27ClO5. Formula Weight: 394.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml. lambdamax: 229, 276 nm. SMILES: ClCC(O)COC(C=C1)=CC=C1C(C)(C)C2=CC=C(OCC(O)CO)C=C2. InChi Code: InChI=1S/C21H27ClO5/c1-21(2,15-3-7-19(8-4-15)26-13-17(24)11-22)16-5-9-20(10-6-16)27-14-18(25)12-23/h3-10,17-18,23-25H,11-14H2,1-2H3. InChi Key: HDTYUHNZRYZEEB-UHFFFAOYSA-N.