A potent and selective agonist of ERβ (Ki = 1.54 nM; EC50 = 3.61 nM); reduces the viability of patient-derived

Erteberel – 1 mg

Brand:
Cayman
CAS:
533884-09-2
Storage:
-20
UN-No:
Non-Hazardous - /

Erteberel is a potent and selective agonist of estrogen receptor β (ERβ; Ki = 1.54 nM; EC50 = 3.61 nM).{34786} Erteberel reduces the viability of patient-derived, ERβ+ primary glioblastoma (GBM) cells, significantly reducing in vitro colony formation and inducing apoptosis.{34787} It induces G2/M arrest and sensitizes GBM cells to the chemotherapeutic agents cisplatin (Item No. 13119), lomustine, and temozolomide (Item No. 14163) in vitro. Treatment with erteberel reduces GBM progression in and increases survival of orthotopic and syngeneic GBM mouse models. Erteberel also induces dose-dependent reduction in prostate weight with no effect on levels of circulating testosterone (Item Nos. 15645 | ISO60154) or dihydrotestosterone (Item No. 15874) in a rat model of benign prostatic hyperplasia (BPH).{34786} Formulations containing erteberel have been tested in phase II clinical trials for treatment of BPH in healthy men.{34785}  

 

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Description

A potent and selective agonist of ERβ (Ki = 1.54 nM; EC50 = 3.61 nM); reduces the viability of patient-derived, ERβ+ primary GBM cells; reduces in vitro colony formation and induces apoptosis; induces G2/M arrest and sensitizes GBM cells to chemotherapeutic agents in vitro; reduces GBM progression in and increases survival of orthotopic and syngeneic GBM mouse models; induces dose-dependent reduction in prostate weight with no effect on levels of circulating testosterone or dihydrotestosterone in a rat model of BPH

Formal name: (3aS,4R,9bR)-1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-cyclopenta[c][1]benzopyran-8-ol

Synonyms:  LY500307

Molecular weight: 282.3

CAS: 533884-09-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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