Rubone
Based on 1 Customer Validation
Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.1%
- CAS 番号: 73694-15-2
- 分子式: C20H22O7
- 分子量:374.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
Rubone (0-60 μM) exhibits significantly high cytotoxicity in DU145-TXR and PC3-TXR cells, suggesting that Rubone has stronger anticancer effect in advanced prostate cancer cells, which has lower miR-34a expression[3].
Rubone (5, 10 uM; 48 h) significantly reverses the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines[3].
Rubone (5, 10 uM; 48 h) upregulates miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner[3].
Rubone (5 μM; for 2 weeks) and PTX (for 2 weeks) combination therapy inhibit PC3-TXR cell growth and sphere formation in 3D model, including 3D on top and hanging drop model. Rubone and PTX combination therapy inhibit cell invasion, migration, and cancer stem-like cells (CSCs) population in a p53-independent pathway. Rubone monotherapy or Rubone and PTX combination significantly enhances TAp73 and Elk-1 expression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145, PC3, PTX resistant DU145-TXR, PC3-TXR, LNCaP, LNCaP developed C4-2 cells
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Concentration:0-60 μM
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Incubation Time:
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Result:Exhibited significantly higher cytotoxicity in DU145-TXR and PC3-TXR cells.
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Cell Line:DU145-TXR and PC3-TXR cell lines
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Concentration:5, 10 uM
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Incubation Time:48 h
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Result:Significantly reversed the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines, including E-cadherin, SIRT1, and Cyclin D1, whereas E-cadherin expression was not reversed in DU145-TXR cell line.
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Cell Line:DU145-TXR and PC3-TXR cell lines
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Concentration:5, 10 uM
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Incubation Time:48 h
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Result:Upregulated miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8 weeks old male nude mice transfected prostate cancer cells[3]
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Dosage:20 mg/kg or 10 mg/kg for each drug (PTX and Rubone) loaded PEG-PCD micelles
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Administration:Intravenously for five doses every other day
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Result:Had little effect on body weight loss and inhibited tumor growth.
Monotherapy or combination therapy with PTX significantly upregulated miR-34a expression in tumor.
Alone or with PTX significantly reversed E-cadherin, Cyclin D1, and SIRT1 expression.
化学情報
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CAS 番号 73694-15-2
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性状 Solid
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分子量 374.38
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分子式 C20H22O7
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Color Light yellow to yellow
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SMILES
O=C(/C=C/C1=CC(OC)=C(C=C1OC)OC)C2=C(C=C(C=C2O)OC)OC
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Structure Classification
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 2 mg/mL (5.34 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Español - ES (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zhangang Xiao, et al. Small molecule targeting miR-34a for cancer therapy. Mol Cell Oncol. 2015 Feb 24;2(1):e977160. [Content Brief]
[2]. Lu Zhang, et al. MicroRNA-34 family: a potential tumor suppressor and therapeutic candidate in cancer. J Exp Clin Cancer Res. 2019 Feb 4;38(1):53. [Content Brief]
[3]. Di Wen, et al. Micellar Delivery of miR-34a Modulator Rubone and Paclitaxel in Resistant Prostate Cancer. Cancer Res. 2017 Jun 15;77(12):3244-3254. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6711 mL | 13.3554 mL | 26.7108 mL | 66.7771 mL |
| 5 mM | 0.5342 mL | 2.6711 mL | 5.3422 mL | 13.3554 mL |