Prinaberel
Based on 4 publication(s) in Google Scholar
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.
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- Reinheit: 98.05%
- CAS. Nr.: 524684-52-4
- Formel: C15H10FNO3
- Molecular Weight:271.24
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Prinaberel
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Biologische Aktivität
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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) |
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.
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Cell Line:A431 cells
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Concentration:0, 20, 40 and 60 µM
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Incubation Time:24 hours
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Result:Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.
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Cell Line:SKOV-3, A2780CP or OVCAR-3 cells
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Concentration:0.01, 0.1 and 10 µM
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Incubation Time:24-48 hours
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Result:Showed significantly inhibitory effect on cell proliferation.
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.
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Animal Model:Six- to eight-weeks-old SKH-1 hairless female mice[2]
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Dosage:2 mg/mouse in 200µl ethanol
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Administration:Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks
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Result:Diminished UVB-induced skin tumor development in SKH-1 hairless mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 524684-52-4
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Appearance Solid
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Molecular Weight 271.24
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Formel C15H10FNO3
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Color White to gray
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SMILES
OC1=CC(C=C)=C(OC(C2=CC=C(O)C(F)=C2)=N3)C3=C1
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Synonyms
ERB-041
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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ACS Nano
Clinically Validated Leptin Receptor as a Target for Liposomal Delivery of Metformin in Endometriosis Therapy. [Abstract]2026 May 12;20(18):13542-13559. PMID: 42054534 -
BMC Med
NLRC5 exerts anti-endometriosis effects through inhibiting ERβ-mediated inflammatory response. [Abstract]2024 Sep 2;22(1):351. PMID: 39218863 -
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Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040. [Content Brief]
[2]. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014;7(2):186-198. [Content Brief]
[3]. Chan KKL, et al. Estrogen receptor modulators genistein, daidzein and ERB-041 inhibit cell migration, invasion, proliferation and sphere formation via modulation of FAK and PI3K/AKT signaling in ovarian cancer. Cancer Cell Int. 2018;18:65. Published 2018 May 1. [Content Brief]
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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