1. Vitamin D Related/Nuclear Receptor Stem Cell/Wnt Apoptosis
  2. Estrogen Receptor/ERR Wnt Apoptosis
  3. Prinaberel

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.

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

Prinaberel Chemical Structure

Prinaberel Chemical Structure

CAS No. : 524684-52-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 162 In-stock
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Based on 2 publication(s) in Google Scholar

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2 Publications Citing Use of MCE Prinaberel

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Description

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis[1][2][3].

IC50 & Target[1]

hERβ

5.4 nM (IC50)

rat ERβ

3.1 nM (IC50)

mouse ERβ

3.7 nM (IC50)

hERα

1200 nM (IC50)

mouse ERα

750 nM (IC50)

rat ERα

620 nM (IC50)

In Vitro

Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation[2].
Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells[2].
Prinaberel (0.01-10 µM) inhibits cell proliferation in a dose- and time-dependent manner[3].
Prinaberel (10 µM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis[3].

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

Western Blot Analysis[2]

Cell Line: A431 cells
Concentration: 0, 20, 40 and 60 µM
Incubation Time: 24 hours
Result: Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.

Cell Proliferation Assay[3]

Cell Line: SKOV-3, A2780CP or OVCAR-3 cells
Concentration: 0.01, 0.1 and 10 µM
Incubation Time: 24-48 hours
Result: Showed significantly inhibitory effect on cell proliferation.
In Vivo

Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice[2].
Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling[2].

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

Animal Model: Six- to eight-weeks-old SKH-1 hairless female mice[2]
Dosage: 2 mg/mouse in 200µl ethanol
Administration: Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks
Result: Diminished UVB-induced skin tumor development in SKH-1 hairless mice.
Clinical Trial
Molecular Weight

271.24

Formula

C15H10FNO3

CAS No.
Appearance

Solid

Color

White to gray

SMILES

OC1=CC(C=C)=C(OC(C2=CC=C(O)C(F)=C2)=N3)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (147.47 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 3.6868 mL 18.4339 mL 36.8677 mL
5 mM 0.7374 mL 3.6868 mL 7.3735 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (18.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (18.43 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6868 mL 18.4339 mL 36.8677 mL 92.1693 mL
5 mM 0.7374 mL 3.6868 mL 7.3735 mL 18.4339 mL
10 mM 0.3687 mL 1.8434 mL 3.6868 mL 9.2169 mL
15 mM 0.2458 mL 1.2289 mL 2.4578 mL 6.1446 mL
20 mM 0.1843 mL 0.9217 mL 1.8434 mL 4.6085 mL
25 mM 0.1475 mL 0.7374 mL 1.4747 mL 3.6868 mL
30 mM 0.1229 mL 0.6145 mL 1.2289 mL 3.0723 mL
40 mM 0.0922 mL 0.4608 mL 0.9217 mL 2.3042 mL
50 mM 0.0737 mL 0.3687 mL 0.7374 mL 1.8434 mL
60 mM 0.0614 mL 0.3072 mL 0.6145 mL 1.5362 mL
80 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1521 mL
100 mM 0.0369 mL 0.1843 mL 0.3687 mL 0.9217 mL
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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.

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Prinaberel
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HY-14933
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