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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
BMH-21 (BMH 21; BMH21) is a novel and potent DNA intercalator with potential antineoplastic activity. It acts by binding to ribosomal DNA and inhibiting RNA polymerase I (Pol I) transcription. BMH-21 intercalated into dsDNA and exhibited a preference for binding to DNA sequences rich in GCs. With its broad range of cytotoxic effects on human cancer cell lines and its p53-independent action, BMH-21 is frequently used as a mediator of various cytotoxic drugs. By attaching to ribosomal (r) DNA, BMH-21 blocked RNA polymerase I (Pol I) transcription and degraded RPA194, the major catalytic subunit of Pol I.
Targets |
DNA
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ln Vitro |
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ln Vivo |
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Cell Assay |
The cells are kept in a humidified environment with 5% CO2 at 37 °C. The culture medium used for U2OS osteosarcoma cells contains 15% fetal bovine serum in addition to DMEM. In triplicate, cells are plated in 96-well plates at a density of 10,000 cells per well, and the compounds are then incubated for 48 hours. Using the WST-1 cell proliferation reagent, viability is assessed.
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Animal Protocol |
6-week old athymic NCr nu/nu mice, with HCT116 colorectal carcinoma xenograft
50 mg/kg Intraperitoneal injection, daily, for 6 days |
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References |
Molecular Formula |
C21H20N4O2
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Molecular Weight |
360.41
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Exact Mass |
362.17
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Elemental Analysis |
C, 69.59; H, 6.12; N, 15.46; O, 8.83
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CAS # |
896705-16-1
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CN(C)CCNC(=O)C1=CC=CN2C1=NC3=CC4=CC=CC=C4C=C3C2=O
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InChi Key |
BXYDVWIAGDJBEC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H20N4O2/c1-24(2)11-9-22-20(26)16-8-5-10-25-19(16)23-18-13-15-7-4-3-6-14(15)12-17(18)21(25)27/h3-8,10,12-13H,9,11H2,1-2H3,(H,22,26)
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Chemical Name |
N-[2-(dimethylamino)ethyl]-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
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Synonyms |
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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 |
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | |
5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | |
10 mM | 0.2775 mL | 1.3873 mL | 2.7746 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.
BMH-21 Inhibits Replication and Viability of Cancer cells In Vitro and Tumor Growth In Vivo. Cancer Cell . 2014 Jan 13;25(1):77-90. td> |
Binding and Modeling of BMH-21 with GC-rich DNA. Cancer Cell . 2014 Jan 13;25(1):77-90. td> |
BMH-21 Binds rDNA Sequences in GC-content Dependent Mannerand Inhibits rRNA Synthesis In Vitro. Cancer Cell . 2014 Jan 13;25(1):77-90. td> |
BMH-21 Represses rRNA Synthesis and Causes Segregation of Nucleolar Proteins. Cancer Cell . 2014 Jan 13;25(1):77-90. td> |
BMH-21 acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation. Oncotarget . 2014 Jun 30;5(12):4361-9. td> |
BMH-21 does not protect from activation of DNA damage signaling. Oncotarget . 2014 Jun 30;5(12):4361-9. td> |
BMH-21 derivative LI-216 activates DNA damage response. Oncotarget . 2014 Jun 30;5(12):4361-9. td> |