PRODUCT INFORMATION Erteberel Item No. 22130 OH CAS Registry No.: 533884-09-2

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

Synonym: LY500307 O MF: C18H18O3 H FW: 282.3 Purity: ≥98% UV/Vis.: λmax: 225 nm Supplied as: A crystalline solid Storage: -20°C OH Stability: ≥2 years

Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis.

Laboratory Procedures

Erteberel is supplied as a crystalline solid. A stock solution may be made by dissolving the erteberel in the solvent of choice. Erteberel is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of erteberel in these solvents is approximately 30 mg/ml.

Description

Erteberel is a potent and selective agonist of receptor β (ERβ; Ki = 1.54 nM; 1 + EC50 = 3.61 nM). Erteberel reduces the viability of patient-derived, ERβ primary (GBM) cells, 2 significantly reducing in vitro colony formation and inducing apoptosis. 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 (Item Nos. 15645 | ISO60154) or (Item No. 15874) in a rat model of benign prostatic hyperplasia (BPH).1 Formulations containing erteberel have been tested in phase II clinical trials for treatment of BPH in healthy men.3

References

1. Norman, B.H., Dodge, J.A., Richardson, T.I., et al. Benzopyrans are selective beta agonists with novel activity in models of benign prostatic hyperplasia. J. Med. Chem. 49(21), 6155-6157 (2006). 2. Sareddy, G.R., Li, X., Liu, J., et al. Selective estrogen receptor β agonist LY500307 as a novel therapeutic agent for glioblastoma. Sci. Rep. 6:24185, (2016). 3. Roehrborn, C.G., Spann, M.E., Myers, S.L., et al. agonist LY500307 fails to improve symptoms in men with enlarged prostate secondary to benign prostatic hypertrophy. Prostate Cancer Prostatic Dis. 18(1), 43-48 (2015).

WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897

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