| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary targets of 9-Hydroxyellipticine HCl are topoisomerase II (Topo II) and the ryanodine receptor (RyR). Topo II is a nuclear enzyme that catalyzes the transient breaking and rejoining of DNA double strands, which is essential for DNA replication, transcription, and chromosome segregation. By inhibiting Topo II, 9-Hydroxyellipticine HCl stabilizes the enzyme-DNA cleavage complex, leading to DNA double-strand breaks and ultimately cell death. The compound also inhibits RyR, a calcium channel in the sarcoplasmic reticulum, which may contribute to its effects on cellular calcium homeostasis.
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| ln Vitro |
In the range of 0.1 to 100 μM, 9-hydroxyellipticine (9HE) preferentially suppresses the phosphorylation of the p53 protein in Lewis lung carcinoma and the human colon cancer cell line SW480 [4]. This effect is concentration-dependent.
In vitro, 9-Hydroxyellipticine HCl demonstrates potent cytotoxicity against various cancer cell lines. It inhibits the growth of HeLa S-3 cells with an IC50 of 1.6 μM and 293T cells with an IC50 of 1.2 μM. The compound's activity is mediated primarily through the inhibition of Topo II. It also exhibits antioxidant activity. Its potency against cancer cell lines makes it a valuable tool for studying Topo II inhibition and its effects on cancer cell proliferation. However, detailed mechanistic studies are not extensively reported in the available literature. |
| ln Vivo |
In mouse bone marrow cells, 9-hydroxyellipticine (5 or 10 mg/kg, intraperitoneally) induces chromosome aggregation and sister chromatid exchange [1].
In vivo data for 9-Hydroxyellipticine HCl are limited in the available literature. Based on its in vitro antitumor activity, the compound has potential for in vivo efficacy in cancer models. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical. |
| Enzyme Assay |
In vitro enzyme assays for 9-Hydroxyellipticine HCl typically involve measuring its inhibition of topoisomerase II activity. The enzyme is incubated with a DNA substrate (e.g., supercoiled plasmid DNA) in the presence of varying concentrations of the compound. The reaction is stopped, and the DNA is analyzed by agarose gel electrophoresis to detect the formation of linear or relaxed DNA, which indicates Topo II activity. The compound's ability to inhibit Topo II-mediated DNA relaxation or decatenation is assessed.
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| Cell Assay |
Cellular assays for 9-Hydroxyellipticine HCl are performed in various cancer cell lines. Cells are treated with various concentrations of the compound, and cell viability is assessed using assays such as MTT, CCK-8, or resazurin reduction. The compound's cytotoxicity is expressed as the IC50 for inhibition of cell growth. Additional assays, such as flow cytometry for apoptosis or cell cycle analysis, may be performed to study the mechanism of cell death.
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| Animal Protocol |
Animal/Disease Models: 3- to 5-month-old C57B1/6 male mice [1].
Doses: 5 or 10 mg/kg. Management: Intellectual Property. Experimental Results: Caused chromosome aggregation, chromatid aberrations and micronucleus formation in mouse bone marrow cells. In vivo animal studies with 9-Hydroxyellipticine HCl are not extensively documented in the available literature. Based on its antitumor activity, potential in vivo models could include xenograft models in mice, where human cancer cells are implanted subcutaneously. In such studies, 9-Hydroxyellipticine HCl would be administered intraperitoneally or intravenously, and tumor growth would be monitored. However, specific protocols are not detailed in the available sources. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for 9-Hydroxyellipticine HCl are not extensively reported. The compound is a small molecule with a molecular weight that is not specified in the available literature. It is cell-permeable, indicating that it can cross cellular membranes. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
9-Hydroxyellipticine HCl has been studied for its antitumor activity. However, comprehensive toxicology data for this compound are not extensively reported. As a Topo II inhibitor, it may have genotoxic potential, as Topo II inhibitors can cause DNA damage. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
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| Additional Infomation |
9-Hydroxyellipticine HCl is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying topoisomerase II inhibition and its effects on cancer cells. The compound is used to study the mechanisms of Topo II inhibitors, to screen for potential anticancer agents, and to investigate the role of Topo II in DNA replication and cell division. It is also used to study the ryanodine receptor and calcium signaling.
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| Molecular Formula |
C17H14N2O
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|---|---|
| Molecular Weight |
262.31
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| Exact Mass |
298.087
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| CAS # |
52238-35-4
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| Related CAS # |
51131-85-2;52238-35-4 (HCl);58447-24-8 (methiodide);
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| PubChem CID |
148569
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| Appearance |
Yellow to orange solid powder
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| Density |
1.349g/cm3
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| Boiling Point |
557.7ºC at 760mmHg
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| Flash Point |
291.1ºC
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| LogP |
4.993
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
21
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| Complexity |
374
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DLDKVFOKLGPVBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N2O.ClH/c1-9-14-8-18-6-5-12(14)10(2)17-16(9)13-7-11(20)3-4-15(13)19-17;/h3-8,19-20H,1-2H3;1H
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| Chemical Name |
5,11-dimethyl-6H-pyrido[4,3-b]carbazol-9-ol hydrochloride
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| Synonyms |
9-hydroxyellipticine HCl 9-Hydroxyellipticin9-hydroxyellipticine hydrochloride Hydroxyellipticine NSC 210717 IGIG929 IGIG-929 IGIG 929LS133324 LS 133324 LS-133324
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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 | 3.8123 mL | 19.0614 mL | 38.1228 mL | |
| 5 mM | 0.7625 mL | 3.8123 mL | 7.6246 mL | |
| 10 mM | 0.3812 mL | 1.9061 mL | 3.8123 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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