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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
Antibiotic DC 81 demonstrates cytotoxicity at IC50 values of 4.4 μM, 18.5 μM, 31.0 μM, and 41.5 μM for the human melanoma cell lines B16, A375, A2058, and RPMI7951, respectively[1][2]. Through its electrophilic carbinolamine functionality at N10–C11, the antibiotic DC 81 demonstrates its biological action by covalently attaching to the N2 of guanine in the minor groove of DNA[1]. Apoptosis dependent on mitochondria is induced by the antibiotic DC 81 (4 μM, 24 h)[2].
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ln Vivo |
In tumor-bearing animals, Antibiotic DC 81 (0–10 mg/kg, ip, at days 4, 7, 10, and 13 following tumor cell injection) reduces the tumor burden; however, Antibiotic DC 81 at 10 mg/kg severely affects liver and heart muscle function[2].
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Cell Assay |
Apoptosis Analysis[2]
Cell Types: B16 melanoma cells Tested Concentrations: 4 μM Incubation Duration: 24 h Experimental Results: Induced mitochondria dependent apoptosis. |
Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice (8-12 weeks old, B16 cells were injected into the tail veins of mice)[2]
Doses: 0.1, 1, 10 mg/kg Route of Administration: ip, at day 4, 7, 10, 13 after tumor cell injection Experimental Results: Substantially diminished the tumor burden by 20% at 1 mg/kg. DC- 81 at 10 mg/kg induced an 8-10-fold increase of GPT and a 6-8-fold increase in CPK, which indicated severe impaired liver function and muscle damage. Did not impair significant renal function as demonstrated by serum creatinine. |
References |
[1]. Hu WP, et al. Biological evaluation of an antibiotic DC-81-indole conjugate agent in human melanoma cell lines. Kaohsiung J Med Sci. 2003 Jan;19(1):6-12.
[2]. Lee CH, et al. Pyrrolo[2,1-c][1,4]benzodiazepine and indole conjugate (IN6CPBD) has better efficacy and superior safety than the mother compound DC-81 in suppressing the growth of established melanoma in vivo. Chem Biol Interact. 2009 Aug 14;180(3):360-7. |
Molecular Formula |
C13H14N2O3
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Molecular Weight |
246.26
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CAS # |
81307-24-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
OC1C(OC)=CC2C(=O)N3CCCC3C=NC=2C=1
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.0607 mL | 20.3037 mL | 40.6075 mL | |
5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL | |
10 mM | 0.4061 mL | 2.0304 mL | 4.0607 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.