2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Erteberel

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. Erteberel has anti-tumor activities.

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Erteberel Chemical Structure

Erteberel Chemical Structure

CAS No. : 533884-09-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 590 In-stock
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10 mM * 1 mL in DMSO USD 590 In-stock
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1 mg USD 190 In-stock
5 mg USD 550 In-stock
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Based on 2 publication(s) in Google Scholar

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Erteberel Related Antibodies

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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. Erteberel has anti-tumor activities[1][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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Erteberel Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Off-white to light brown

SMILES

OC1=CC=C2C([C@@](CCC3)([H])[C@@]3([H])[C@H](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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.87%

COA (249 KB) HNMR (176 KB) RP-HPLC (121 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5420 mL 17.7098 mL 35.4195 mL 88.5489 mL
5 mM 0.7084 mL 3.5420 mL 7.0839 mL 17.7098 mL
10 mM 0.3542 mL 1.7710 mL 3.5420 mL 8.8549 mL
15 mM 0.2361 mL 1.1807 mL 2.3613 mL 5.9033 mL
20 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4274 mL
25 mM 0.1417 mL 0.7084 mL 1.4168 mL 3.5420 mL
30 mM 0.1181 mL 0.5903 mL 1.1807 mL 2.9516 mL
40 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2137 mL
50 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7710 mL
60 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
80 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1069 mL
100 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
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Erteberel Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Erteberel533884-09-2LY500307LY 500307LY-500307Estrogen Receptor/ERRInhibitorinhibitorinhibit

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