Berubicin
Based on 1 Customer Validation
Berubicin (RTA 744 free base) is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin can be used in the study of tumors related to the nervous system.
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- 純度: 85.02%
- CAS 番号: 677017-23-1
- 分子式: C34H35NO11
- 分子量:633.64
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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NF-κB |
Caspase 3 |
Caspase-9 |
Berubicin (0.1-10 μM, 0-5 d) is more effective than Doxorubicin (Dox) in inhibiting SH-SY5Y cell growth[2].
Berubicin (0-10 μM, 0-48 h) induces apoptosis at the lower drug concentrations through caspase-9 and -3-dependent pathways and activating NF-κB, while other mechanisms of cell death may predominate at higher concentrations in SH-SY5Y cells[2].
Berubicin (0-100 μM, 24 h) inhibits three AML cell lines K562, KBM-3, OCIM2 and KBM-5 cells with IC50s of 0.18, < 0.05, < 0.05 μg/mL and 0.5 μM, and induces cell apoptosis in cultured human acute lymphoblastic leukemia (ALL) CEM cells at 0.05 μM[3][4].
Berubicin (0-10 μM, 0-8 h) is more active than Dox in inhibiting DNA synthesis (IC50 = 0.2 μM), activating NF-κB and degradation of IkBα of KBM-5 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:0.05, 0.5 and 5 μM
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Incubation Time:48 h
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Result:Induced significantly higher apoptosis at 500 nM than Dox, but higher concentrations of the drug reduced the apoptosis-inducing effect.
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Cell Line:SH-SY5Y cells
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Concentration:0, 0.1, 1 and 10 μM
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Incubation Time:0, 0.5, 1, 2, 4, 6, 8, 12, 24 h
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Result:Observed a caspase-9 cleavage band as early as 0.5 h after drug treatment and accumulated to highest levels after 12 h, and caspase-3 cleavage was seen as early as 8 h.
Did not express caspase 8, and there was no increase or decrease in caspase 7 expression.
Significantly increased p53 levels, whereas Dox had no such effect and p21 expression increased with increased p53.
Significantly reduced mitochondrial AIF and nuclear AIF accumulation increases over time.
Showed 50 times more potent than Dox in activating NF-κB.
Downregulated the expression of IκBα, Bcl-w, Bcl-XL and cyclin D1.
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Cell Line:KBM-5 cells
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Concentration:0, 0.1, 1, 10 μM
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Incubation Time:0, 5, 10, 15, 30, 60, 120, 240, 480 min
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Result:Was most active, reaching maximum activation in activating NF-kβ and degradation of IkBαat a 1 μM concentration, and Doxorubicin least active, reaching maximum at 50 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 677017-23-1
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性状 Solid
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分子量 633.64
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分子式 C34H35NO11
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Color Purple to purplish red
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SMILES
OC1=C2C([C@@]([H])(O[C@H]3C[C@H](N)[C@H](OCC4=CC=CC=C4)[C@H](C)O3)C[C@@](C(CO)=O)(O)C2)=C(O)C5=C1C(C6=CC=CC(OC)=C6C5=O)=O
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別名
RTA 744 free base; WP 744 free base; WP 769
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (157.82 mM; Need ultrasonic; 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 (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- 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
[3]. Faderl S, Estrov Z, Kantarjian HM, Harris D, Van Q, Fokt I, Przewloka T, Godlewski C, Woynarowski JM, Priebe W. WP744, a novel anthracycline with enhanced proapoptotic and antileukemic activity. Anticancer Res. 2001 Nov-Dec;21(6A):3777-84. PMID: 11911247. [Content Brief]
[4]. Ashikawa K, et al. Evidence that activation of nuclear factor-kappaB is essential for the cytotoxic effects of doxorubicin and its analogues. Biochem Pharmacol. 2004 Jan 15;67(2):353-64. [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 | 1.5782 mL | 7.8909 mL | 15.7818 mL | 39.4546 mL |
| 5 mM | 0.3156 mL | 1.5782 mL | 3.1564 mL | 7.8909 mL | |
| 10 mM | 0.1578 mL | 0.7891 mL | 1.5782 mL | 3.9455 mL | |
| 15 mM | 0.1052 mL | 0.5261 mL | 1.0521 mL | 2.6303 mL | |
| 20 mM | 0.0789 mL | 0.3945 mL | 0.7891 mL | 1.9727 mL | |
| 25 mM | 0.0631 mL | 0.3156 mL | 0.6313 mL | 1.5782 mL | |
| 30 mM | 0.0526 mL | 0.2630 mL | 0.5261 mL | 1.3152 mL | |
| 40 mM | 0.0395 mL | 0.1973 mL | 0.3945 mL | 0.9864 mL | |
| 50 mM | 0.0316 mL | 0.1578 mL | 0.3156 mL | 0.7891 mL | |
| 60 mM | 0.0263 mL | 0.1315 mL | 0.2630 mL | 0.6576 mL | |
| 80 mM | 0.0197 mL | 0.0986 mL | 0.1973 mL | 0.4932 mL | |
| 100 mM | 0.0158 mL | 0.0789 mL | 0.1578 mL | 0.3945 mL |
Berubicin 関連分類
HY-14942 関連分類
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