普林贝瑞
- CAS号:524684-52-4
- 英文名:Prinaberel
- 中文名:普林贝瑞
- CBNumber:CB21509128
- 分子式:C15H10FNO3
- 分子量:271.24
- MOL File:524684-52-4.mol
- 熔点 :250-252 ºC
- 沸点 :451.6±45.0 °C(Predicted)
- 密度 :1.413
- 储存条件 :room temp
- 溶解度 :DMSO: ≥25mg/mL
- 形态 :powder
- 酸度系数(pKa) :7.50±0.20(Predicted)
- 颜色 :white to tan
- InChIKey :MQIMZDXIAHJKQP-UHFFFAOYSA-N
普林贝瑞性质、用途与生产工艺
- 生物活性 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)。
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靶点
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 )
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体外研究
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. -
体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-14933
- 产品名称：Prinaberel
- CAS编号：
- 包装：1 mg
- 价格：383元
- 更新日期：2024/11/08
- 产品编号：HY-14933
- 产品名称：Prinaberel
- CAS编号：
- 包装：5 mg
- 价格：843元
- 公司名称：TORONTO
- 联系电话：--
- 电子邮件：info@trc-canada.com
- 国家：加拿大
- 产品数：6038
- 优势度：71
