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Erteberel (Synonyms: LY500307)

Cat. No.: HY-18295
Handling Instructions

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.

For research use only. We do not sell to patients.

Erteberel Chemical Structure

Erteberel Chemical Structure

CAS No. : 533884-09-2

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  • Biological Activity

  • Technical Information

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  • References

Description

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].

IC50 & Target

ERβ

1.54 nM (Ki)

ERβ

3.61 nM (EC50)

In Vitro

Treatment with Erteberel (0.25, 0.5, 1, 2, 4, 6, 8, and 10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2].

ERβ agonists promote apoptosis of GBM cells. It modulated several pathways related to apoptosis, cell cycle, and DNA damage response[2].

Erteberel (0-1000 μM) sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide[2].

Cell Viability Assay[2]

Cell Line: U87, U251,T98G and normal astrocytes
Concentration: 0.25, 0.5, 1, 2, 4, 6, 8, and 10 μM
Incubation Time: 72 h
Result: Treatment with LY500307 significantly reduces the viability of various GBM cell lines in a dose-dependent manner. In contrast, viability of normal astrocytes is not affected at the tested doses, suggesting that LY500307 has tumor cell–specific activity[2].
In Vivo

Erteberel (5 mg/Kg body weight/day, oral, 28 days) treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model[2].

Erteberel (5 mg/Kg body weight/day, oral, 40-50 days) treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model[2].

Animal Model: Athymic mice (5-7 weeks) inoculated with OVCAR-3 cells[2]
Dosage: 5mg/Kg body weight
Administration: Oral, 28 days
Result: Immunohistochemical analysis reveals that LY500307 treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells[2].
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5420 mL 17.7098 mL 35.4195 mL
5 mM 0.7084 mL 3.5420 mL 7.0839 mL
10 mM 0.3542 mL 1.7710 mL 3.5420 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

282.33

Formula

C₁₈H₁₈O₃

CAS No.

533884-09-2

SMILES

OC1=CC=C2C([[email protected]@](CCC3)([H])[[email protected]@]3([H])[[email protected]](C4=CC=C(O)C=C4)O2)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Erteberel
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Erteberel

Cat. No.: HY-18295