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产品描述： 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 |
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靶点：
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);Estrogen/progestogenReceptor |
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. |
参考文献：
1. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040. 2. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014;7(2):186-198. 3. Chan KKL, et al. Estrogen receptor modulators genistein, daidzein and ERB-041 inhibit cell migration, invasion, proliferation and sphere formation via modulation of FAK and PI3K/AKT signaling in ovarian cancer. Cancer Cell Int. 2018;18:65. Published 2018 |
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溶解性：
Soluble in DMSO |
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保存条件：
RT |
配置溶液浓度参考：
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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 |
| 50 mM |
0.074 ml |
0.369 ml |
0.737 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京