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  3. Prinaberel

Prinaberel (Synonyms: ERB-041)

Cat. No.: HY-14933 Purity: 98.62%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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50 mg USD 648 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (147.47 mM)

*"≥" 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
10 mM 0.3687 mL 1.8434 mL 3.6868 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Prinaberel
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