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  3. Erteberel

Erteberel (Synonyms: LY500307)

Cat. No.: HY-18295 Purity: >99.0%
Handling Instructions

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist 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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10 mM * 1  mL in DMSO USD 823 Ask For Quote & Lead Time
1 mg USD 265 Ask For Quote & Lead Time
5 mg USD 795 Ask For Quote & Lead Time

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Description

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist 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 (0.25-10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2].

Erteberel promotes apoptosis of GBM cells. Erteberel 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 Erteberel 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 Erteberel 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, daily for 28 days
Result: Immunohistochemical analysis reveals that Erteberel treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells[2].
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (106.26 mM)

*"≥" means soluble, but saturation unknown.

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

Purity: >99.0%

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Keywords:

ErteberelLY500307LY 500307LY-500307Estrogen Receptor/ERRInhibitorinhibitorinhibit

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