S85645 |
ERB 041 |
源葉(MedMol) | 98% |
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- 產(chǎn)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
- 靶點(diǎn): 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
- 體內(nèi)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.
- 參考文獻(xiàn):
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
- 溶解性: Soluble in DMSO
- 保存條件: RT
- 配置溶液濃度參考:
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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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)