| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Topoisomerase II 0.98 μM (IC50)
Topoisomerase II (a nuclear enzyme essential for DNA replication, transcription, and chromosome segregation) |
|---|---|
| ln Vitro |
Topoisomerase II inhibitor 20 TFA demonstrates potent inhibition of topoisomerase II with an IC50 of 0.98 uM. It induces apoptosis in cancer cell lines and exhibits broad-spectrum anticancer activity, suggesting it may be effective against multiple cancer types. Detailed in vitro efficacy across different cell lines is not provided beyond this general description.
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| ln Vivo |
Currently, no in vivo data are available for Topoisomerase II inhibitor 20 TFA. Its reported broad-spectrum anticancer activity suggests potential for future in vivo validation, but as of now, no animal studies or efficacy data in living systems have been published.
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| Enzyme Assay |
Typical Topoisomerase II inhibition assay: incubate recombinant human topoisomerase IIalpha with kinetoplast DNA (kDNA) in assay buffer (50 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, 0.5 mM DTT, 1 mM ATP, 30 ug/mL BSA) at 37degC for 30 min. After adding test compound, reactions are stopped with SDS/Proteinase K. Decatenated kDNA products are separated by agarose gel electrophoresis and visualized by ethidium bromide staining.
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| Cell Assay |
Cell line: Any cancer cell line (e.g., HeLa, MCF-7, A549) cultured in appropriate media with 10% FBS. Treatment: cells seeded in 96-well plates, incubated with a dose range of Topoisomerase II inhibitor 20 TFA (0.01-100 uM) for 48-72 h. Viability: MTT assay (add 5 mg/mL MTT, incubate 4 h, dissolve formazan in DMSO, read OD570). Apoptosis: Annexin V-FITC/PI staining, flow cytometry.
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| Animal Protocol |
No published in vivo data were found. A general protocol for evaluating Topoisomerase II inhibitors in vivo: establish subcutaneous xenografts of cancer cells (e.g., A549 or HCT116) in nude mice (5×10⁶ cells/injection). When tumors reach ~100-150 mm3, mice are randomized to receive Topo II inhibitor 20 TFA (e.g., 10-50 mg/kg, IP or oral) or vehicle daily for 2-3 weeks. Tumor volume measured twice weekly.
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| ADME/Pharmacokinetics |
No PK data were found. Typical studies for a Topo II inhibitor would involve IV/oral administration to rodents (e.g., 5-10 mg/kg IV, 20-50 mg/kg PO), plasma collection, LC-MS/MS analysis to determine clearance, volume of distribution, terminal half-life (t1/2), oral bioavailability (F%). No such data were reported.
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| Toxicity/Toxicokinetics |
No toxicity data was found. Standard toxicological evaluation would include acute toxicity study in mice (single dose escalation up to 2000 mg/kg) observing for 14 days, and repeat-dose oral toxicity in rats (28 days) with assessment of clinical signs, body weight changes, food consumption, hematology, serum chemistry, and histopathology.
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| References | |
| Additional Infomation |
Topoisomerase II inhibitor 20 TFA is a research-grade small molecule designed to inhibit topoisomerase II, an established anticancer target. Several topoisomerase II inhibitors (e.g., etoposide, doxorubicin) are FDA-approved chemotherapeutics. This compound may serve as a lead for further optimization. It is supplied in TFA salt form for enhanced solubility. Soluble in DMSO at >10 mM.
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| Molecular Formula |
C24H24F5N5O4S
|
|---|---|
| Molecular Weight |
573.54
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| Related CAS # |
Topoisomerase II inhibitor 20
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| Appearance |
Solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 1.7436 mL | 8.7178 mL | 17.4356 mL | |
| 5 mM | 0.3487 mL | 1.7436 mL | 3.4871 mL | |
| 10 mM | 0.1744 mL | 0.8718 mL | 1.7436 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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