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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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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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> |