普林贝瑞
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- CAS号:
- 524684-52-4
- 英文名:
- Prinaberel
- 英文别名:
- ERB 041;PRINABEREL;WAY-202041;Prinaberel (ERB 041);2-(3-Fluoro-4-hydroxyphenyl)-
7-vinylbenzoxazol-5-ol;7-Ethenyl-2-(3-fluoro-4-hydroxyphenyl)-5-benzoxazolol;2-(3-Fluoro-4-hydroxyphenyl)-7-vinylbenzo[d]oxazol-5-ol;5-Benzoxazolol, 7-ethenyl-2-(3-fluoro-4-hydroxyphenyl)-;2-(3-Fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
- 中文名:
- 普林贝瑞
- 中文别名:
- 普林贝瑞;2-(3-氟-4-羟苯基)-7-乙烯基苯并[D]恶唑-5-醇;2-(3-氟-4-羟基苯基)-7-乙烯基-1,3-苯并恶唑-5-醇
- CBNumber:
- CB21509128
- 分子式:
- C15H10FNO3
- 分子量:
- 271.24
- MOL File:
- 524684-52-4.mol
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普林贝瑞化学性质
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熔点:
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250-252 ºC
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沸点:
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451.6±45.0 °C(Predicted)
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密度:
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1.413
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储存条件:
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room temp
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溶解度:
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DMSO: ≥25mg/mL
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形态:
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powder
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酸度系数(pKa):
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7.50±0.20(Predicted)
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颜色:
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white to tan
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InChIKey:
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MQIMZDXIAHJKQP-UHFFFAOYSA-N
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普林贝瑞性质、用途与生产工艺
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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hERβ
5.4 nM (IC
50
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rat ERβ
3.1 nM (IC
50
)
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mouse ERβ
3.7 nM (IC
50
)
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hERα
1200 nM (IC
50
)
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mouse ERα
750 nM (IC
50
)
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rat ERα
620 nM (IC
50
)
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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
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Cell Line:
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A431 cells
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Concentration:
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0, 20, 40 and 60 µM
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Incubation Time:
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24 hours
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Result:
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Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.
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Cell Proliferation Assay
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Cell Line:
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SKOV-3, A2780CP or OVCAR-3 cells
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Concentration:
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0.01, 0.1 and 10 µM
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Incubation Time:
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24-48 hours
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Result:
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Showed significantly inhibitory effect on cell proliferation.
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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.
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Animal Model:
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Six- to eight-weeks-old SKH-1 hairless female mice
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Dosage:
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2 mg/mouse in 200µl ethanol
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Administration:
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Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks
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Result:
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Diminished UVB-induced skin tumor development in SKH-1 hairless mice.
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普林贝瑞
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-14933 | Prinaberel | | 1 mg | 383元 |
| 2024/04/30 | HY-14933 | Prinaberel | | 5 mg | 843元 |
普林贝瑞
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普林贝瑞国内生产厂家
524684-52-4, 普林贝瑞 相关搜索:
- Pharmaceuticals
- Pfizer Compounds
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- Aromatics
- 抑制剂
- 2-(3-氟-4-羟苯基)-7-乙烯基苯并[D]恶唑-5-醇
- 普林贝瑞
- 2-(3-氟-4-羟基苯基)-7-乙烯基-1,3-苯并恶唑-5-醇
- 524684-52-4
- 2-(3-Fluoro-4-hydroxyphenyl)-7-vinylbenzo[d]oxazol-5-ol
- 5-Benzoxazolol, 7-ethenyl-2-(3-fluoro-4-hydroxyphenyl)-
- WAY-202041
- Prinaberel (ERB 041)
- 2-(3-Fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
- PRINABEREL
- 7-Ethenyl-2-(3-fluoro-4-hydroxyphenyl)-5-benzoxazolol
- 2-(3-Fluoro-4-hydroxyphenyl)-
7-vinylbenzoxazol-5-ol
- ERB 041