Prinaberel (ERB-041) 是一种有效的选择性雌激素受体 β (ERβ) 激动剂，对人，大鼠和小鼠 ERβ 的IC50分别为 5.4、3.1 和 3.7 nM。 Prinaberel 对 ERβ 的选择性是 ERα 的 200 倍以上。Prinaberel是有效的皮肤癌化学预防剂，可通过抑制WNT/β-catenin信号通路发挥作用。Prinaberel 诱导卵巢癌细胞凋亡 (apoptosis)。
| 生物活性 | Prinaberel (ERB-041) is a potent and selectiveestrogen receptor(ER) βagonist withIC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouseERβ, respectively. Prinaberel displays >200-fold selectivity forERβoverERα. Prinaberel is a potent skincancerchemopreventive agent that acts by dampening theWNT/β-cateninsignaling pathway. Prinaberel induces ovariancancerapoptosis[1][2][3]. |
| IC50& Target | 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) |
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体外研究
(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].
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. |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 40 mg/mL(147.47 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5 mg/mL (18.43 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (18.43 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 5 mg/mL (18.43 mM); Suspended solution; Need ultrasonic
此方案可获得 5 mg/mL (18.43 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (18.43 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (18.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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