Prinaberel
ERB 041
CAS: 524684-52-4
Molecular Formula: C15H10FNO3
Prinaberel - Names and Identifiers
Prinaberel - Physico-chemical Properties
| Molecular Formula | C15H10FNO3 |
| Molar Mass | 271.24 |
| Density | 1.413 |
| Melting Point | 250-252 ºC |
| Boling Point | 451.6±45.0 °C(Predicted) |
| Solubility | DMSO: ≥25mg/mL |
| Appearance | powder |
| Color | white to tan |
| pKa | 7.50±0.20(Predicted) |
| Storage Condition | room temp |
| In vitro study | Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation. 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. Prinaberel (0.01-10 µM) inhibits cell proliferation in a dose- and time-dependent manner. Prinaberel (10 µM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis. Western Blot Analysis 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 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 study | Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice. 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. Animal Model: Six- to eight-weeks-old SKH-1 hairless female mice 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. |
Prinaberel - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
Prinaberel - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.687 ml | 18.434 ml | 36.868 ml |
| 5 mM | 0.737 ml | 3.687 ml | 7.374 ml |
| 10 mM | 0.369 ml | 1.843 ml | 3.687 ml |
| 5 mM | 0.074 ml | 0.369 ml | 0.737 ml |
Last Update：2024-01-02 23:10:35
Prinaberel - Reference Information
| biological activity | Prinaberel (ERB-041) is an effective selective estrogen receptor β (ERβ) agonist, the IC50 of human, rat and mouse ERβ is 5.4, 3.1 and 3.7 nM respectively. The selectivity of Prinaberel to ERβ is more than 200 times that of ERα. Prinaberel is an effective chemopreventive agent for skin cancer and can play a role by inhibiting WNT/β-catenin signaling pathway. Prinaberel induces apoptosis in ovarian cancer cells (apoptosis). |
| target | hERβ 5.4 nM (IC 50 ) rat ERβ 3.1 nM (IC 50 ) mouse ERβ 3.7 nM (IC 50 ) hERα 1200 nM (IC 50 ) mouse ERα 750 nM (IC 50 ) rat ERα 620 nM (IC 50 ) |
| in vitro study | Prinaberel (ERB-041) (0-60µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation. Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and -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. Prinaberel (0.01-10 m) inhibits cell proliferation in a dose- and time-dependent manner. Prinaberel (10 m; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis. Western Blot Analysis Cell Line: A431 cells Concentration: 0,20, 40 and 60 m Incubation Time: 24 hours Result: reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4. Cell Proliferation Assay 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. |
| Cell Line: | A431 cells SKOV-3, A2780CP or OVCAR-3 cells |
| Concentration: | 0, 20, 40 and 60 µM 0.01, 0.1 and 10 µM |
| Incubation Time: | 24 hours 24-48 hours |
| Result: | Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4. Showed significantly inhibitory effect on cell proliferation. Diminished UVB-induced skin tumor development in SKH-1 hairless mice. |
| in vivo study | Prinaberel (2 mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice. 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 tumour invasiveness via PI3K-AKT pathway and WNT signaling. Animal Model: six-to eight-weeks-old SKH-1 hairless female mice Dosage: 2 mg/mouse in 200 µl ethanol Administration: Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks result: Diminished UVB-induced skin development in SKH-1 hairless mice. |
| Animal Model: | Six- to eight-weeks-old SKH-1 hairless female mice |
| Dosage: | 2 mg/mouse in 200µl ethanol |
| Administration: | Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks |
Last Update：2024-04-09 20:52:54
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CAS: 524684-52-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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Spot supply
Product Name: ERB-041 Visit Supplier Webpage Request for quotationCAS: 524684-52-4
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Prinaberel Visit Supplier Webpage Request for quotationCAS: 524684-52-4
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: Prinaberel Visit Supplier Webpage Request for quotationCAS: 524684-52-4
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: ERB 041 Visit Supplier Webpage Request for quotation
CAS: 524684-52-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 524684-52-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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