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500mg |
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1g |
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2g |
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5g |
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Berbamine 2HCl is a naturally occuring isoquinoline alkaloid found in traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker. It can be used to treat or prevent cardiac arrhythmias, and it may have an impact on the action potential's polarization-repolarization phase, excitability or refractoriness, impulse conduction, or membrane responsiveness within cardiac fibers.
Targets |
Bcr-Abl; NF-κB; CaMKII
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ln Vitro |
Following the down-regulation of IKKα, p-IκBα, caused by berbamine treatment, p65 nuclear localization is then inhibited. This results in an increase in the expression of A20. Due to this, cyclin D1, Bcl-xL, Bid, and survivin, which are downstream targets of NF-κB, are downregulated. KM3 cells are treated with Berbamine at different concentrations for 24, 48, and 72 hours, respectively, to see if it has an effect on myeloma cell growth before MTT assays are used to measure cell viability. The growth of KM3 cells is inhibited by berbamine in a dose- and time-dependent manner; the IC50 values are, respectively, 8.17 μg/mL, 5.09 μg/mL, and 3.84 μg/mL for treatment over 24, 48, and 72 h. A normal hematopoietic cell's IC50 value for berbamine is 185.20 μg/mL at 48 hours, in contrast[1].
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ln Vivo |
Berbamine (BBM) is a natural bisbenzylisoquinoline compound, has been used to treat inflammatory and other diseases since it was isolated from the traditional Chinese herb Berberis amurensis.On a xenograft animal model, Berbamine's anti-tumor properties are assessed. Huh7 (epithelial) and SK-Hep-1 (mesenchymal-like), two liver cancer cell lines, are subcutaneously injected into NOD/SCID mice. On the basis of the tumor weight, the oral Berbamine therapy significantly slows the progression of Huh7 xenografted tumors over time.
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Cell Assay |
MTT assay is used to measure Berbamine's inhibitory effect on KM3 cell growth. Briefly, for 24, 48, or 72 hours, KM3 cells ((8×103 per well) are incubated with increasing concentrations of Berbamine (1-32 μ/mL), followed by a pulse of 20 μL of 5 mg/mL MTT for the final 4 hours. 200 L DMSO is then added to dissolve the formazan crystals. To determine the inhibitory concentration of 50% (IC50), dye absorbance in viable cells is measured at 570 nm[1].
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Animal Protocol |
Mice: The NOD/SCID mice are injected with 5×106 Huh7 cells in 50% Matrigel dissolved in PBS. Each xenograft receives 5×106 SK-Hep-1 cells without the use of Matrigel. After the tumors grow to a diameter of 2 mm, mice are given oral treatments with 100 mg/kg of Berbamine twice daily for 5 days straight. The regimen is carried out once more after two days of withdrawal[2].
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References |
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Molecular Formula |
C₃₇H₄₂CL₂N₂O₆
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Molecular Weight |
681.65
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Exact Mass |
680.2419925
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Elemental Analysis |
C, 65.20; H, 6.21; Cl, 10.40; N, 4.11; O, 14.08
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CAS # |
6078-17-7
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Related CAS # |
Berbamine;478-61-5
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Appearance |
Solid
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SMILES |
CN1CCC2=CC(=C3C=C2[C@@H]1CC4=CC=C(C=C4)OC5=C(C=CC(=C5)C[C@@H]6C7=C(O3)C(=C(C=C7CCN6C)OC)OC)O)OC.Cl.Cl
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InChi Key |
USRXDYNDPPUBSG-KKXMJGKMSA-N
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InChi Code |
InChI=1S/C37H40N2O6.2ClH/c1-38-14-12-24-19-32(41-3)33-21-27(24)28(38)16-22-6-9-26(10-7-22)44-31-18-23(8-11-30(31)40)17-29-35-25(13-15-39(29)2)20-34(42-4)36(43-5)37(35)45-33;;/h6-11,18-21,28-29,40H,12-17H2,1-5H3;2*1H/t28-,29+;;/m0../s1
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Chemical Name |
(1S,14R)-20,21,25-trimethoxy-15,30-dimethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.23,6.18,12.114,18.027,31.022,33]hexatriaconta-3(36),4,6(35),8,10,12(34),18,20,22(33),24,26,31-dodecaen-9-ol;dihydrochloride
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Synonyms |
Berbamine HCl; Berbamine hydrochloride
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~146.7 mM)
Water: ~50 mg/mL (~73.4 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4670 mL | 7.3351 mL | 14.6703 mL | |
5 mM | 0.2934 mL | 1.4670 mL | 2.9341 mL | |
10 mM | 0.1467 mL | 0.7335 mL | 1.4670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
The structural formula of berbamine (molecular weight: 753.80). Acta Pharmacol Sin . 2009 Dec;30(12):1659-65. td> |
Berbamine causes inhibition of translocation of p65 into the nucleus. Acta Pharmacol Sin . 2009 Dec;30(12):1659-65. td> |
Effect of berbamine on the constitutive expression of p65. KM3 cells were treated with 8 μg/mL berbamine for the indicated times, nuclear and whole cell lysates were prepared to check the level of p65 by Western blotting. Acta Pharmacol Sin . 2009 Dec;30(12):1659-65. td> |
Effect of berbamine on cell cycle progression. Acta Pharmacol Sin . 2009 Dec;30(12):1659-65. td> |