| Size | Price | Stock | Qty |
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| 1mg |
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| 1g | |||
| Other Sizes |
| Targets |
Datelliptium chloride hydrochloride targets DNA by intercalation. This intercalation inhibits topoisomerase II activity. It also inhibits mitochondrial complex IV (cytochrome c oxidase). Its anticancer activity is attributed to its DNA-intercalating and topoisomerase II-inhibiting properties.
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| ln Vitro |
In suspension and primary cultures of rat hepatocytes, datelliptium chloride hydrochloride exhibits cytotoxic effects after two hours of treatment[1].
In vitro, Datelliptium chloride hydrochloride intercalates into DNA and inhibits topoisomerase II in a concentration-dependent manner. It also inhibits mitochondrial complex IV. These activities contribute to its anticancer effects in various cancer cell lines. |
| ln Vivo |
In vivo, datelliptium chloride hydrochloride exhibits extensive anticancer efficacy against mice's solid tumors[2]. When a disease is in its early stages, datelliptium chloride hydrochloride (170 mg/kg; IV; for 12 days) has a strong antitumor effect[2]. For solid tumors above leukemia L1210, hydrochloride is specifically cytotoxic[2].
In vivo, Datelliptium chloride hydrochloride is effective against a variety of murine solid tumors. It has been shown to successfully treat numerous solid tumors in mice. It is typically administered at doses such as 170 mg/kg. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Datelliptium chloride hydrochloride involve measuring its inhibition of topoisomerase II activity. These assays typically use purified topoisomerase II enzyme and DNA substrates to assess the compound's ability to inhibit DNA decatenation or relaxation.
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| Cell Assay |
Cytotoxicity is measured using cultured and suspended rat hepatocytes following a brief (2-hour) exposure to datelliptium. In order to assess cytotoxicity following extended exposure, the compound is added one hour after cell plating and incubated for twenty-three hours using rat and human monolayers as well as hepatoma cell lines. In cultured cells, the endpoints assessed are the decrease in intracellular LDH and the MTT test. A colorimetric technique is used to measure the intracellular LDH in the microwell culture plates. The MTT test is carried out according to instructions, with the tetrazolium salt MTT being reduced to formazan by mitochondrial succinate dehydrogenase. Following a two-hour drug treatment, LDH leakage to the medium is used to assess cytotoxicity in the hepatocyte suspension.
In vitro cell-based assays for Datelliptium chloride hydrochloride involve treating cancer cells to assess its effects on cell viability and proliferation. Its DNA-intercalating and topoisomerase II-inhibiting activities are studied in these cellular models. Its effects on mitochondrial function are also assessed. |
| Animal Protocol |
Animal/Disease Models: Mice, colon adenocarcinoma early staged disease model[2]
Doses: 170 mg/ kg Route of Administration: intravenous (iv)injection, for 12 days Experimental Results: demonstrated potent activity against colon adenocarcinoma. In vivo animal experiments for Datelliptium chloride hydrochloride have been conducted in mouse models of solid tumors. The compound is typically administered intraperitoneally or intravenously, and its effects on tumor growth and survival are assessed. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Datelliptium chloride hydrochloride is not provided in the search results. Its properties as a DNA intercalator may influence its distribution and clearance. It is typically administered via injection in preclinical studies.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Datelliptium chloride hydrochloride is not provided in the search results. As a DNA intercalator and topoisomerase II inhibitor, it may have a similar toxicity profile to other anticancer agents in its class, which can include myelosuppression and gastrointestinal toxicity.
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| References |
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| Additional Infomation |
Datelliptium chloride hydrochloride is an anticancer agent derived from ellipticine. It is a DNA intercalator and topoisomerase II inhibitor that is effective against murine solid tumors. It is a research compound that has not been approved for clinical use.
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| Molecular Formula |
C23H29CL2N3O
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|---|---|
| Molecular Weight |
434.4018638134
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| Exact Mass |
433.17
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| CAS # |
157000-76-5
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| Related CAS # |
Datelliptium chloride;105118-14-7
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| PubChem CID |
24844807
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CC[N+]1=CC2=C(C3=C(C(=C2C=C1)C)NC4=C3C=C(C=C4)O)C.Cl.[Cl-]
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| InChi Key |
QLZIAISICLKYOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27N3O.2ClH/c1-5-25(6-2)11-12-26-10-9-18-16(4)23-22(15(3)20(18)14-26)19-13-17(27)7-8-21(19)24-23;;/h7-10,13-14,27H,5-6,11-12H2,1-4H3;2*1H
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| Chemical Name |
2-[2-(diethylamino)ethyl]-5,11-dimethyl-6H-pyrido[4,3-b]carbazol-2-ium-9-ol;chloride;hydrochloride
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| Synonyms |
Datelliptium chloride 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 |
| 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 | 2.3020 mL | 11.5101 mL | 23.0203 mL | |
| 5 mM | 0.4604 mL | 2.3020 mL | 4.6041 mL | |
| 10 mM | 0.2302 mL | 1.1510 mL | 2.3020 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.
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