An androgen receptor antagonist (IC50 = ~6 μM for inhibition of transactivation of the androgen receptor NTD); inhibits androgen-

EPI-001 – 25 mg

Brand:
Cayman
CAS:
227947-06-0
Storage:
-20
UN-No:
Non-Hazardous - /

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).{38581} 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.  

 

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Description

An androgen receptor antagonist (IC50 = ~6 μM for inhibition of transactivation of the androgen receptor NTD); inhibits androgen-, FSK-, and IL-6-induced, as well as ligand-independent, 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; 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; 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; reduces serum PSA and tumor growth in an LNCaP prostate cancer xenograft model in castrated mice when administered at a dose of 50 mg/kg,

Formal name: 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol

Synonyms: 

Molecular weight: 394.9

CAS: 227947-06-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens

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