| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Topoisomerase I Topoisomerase II
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|---|---|
| ln Vitro |
Compound 1a, or topoisomerase I/II inhibitor 2, shows stronger inhibitory efficacy on two human hepatocellular carcinoma cell lines (HuH7, LM9) and excellent anti-proliferative activity in cancer cell lines (0-150 μM; 72 hours)[1]. HuH7 cells show no harm from topoisomerase I/II inhibitor 2 (20 μM; 24 hours); LM9 cells show moderate damage[1]. Huh7 and LM9 cell proliferation is inhibited by topoisomerase I/II inhibitor 2 (1.25-8 μM; 1-2 weeks) in a concentration-dependent manner[1]. In LM9 and HuH7 cells, topoisomerase I/II inhibitor 2 (1.25-8 μM; 24 hours) exhibits a good concentration-dependent inhibitory effect on migration and invasion[1]. In LM9 and HuH7 cells, topoisomerase I/II inhibitor 2 (0–20 μM; 24 hours) can suppress the production of matrix metalloproteinases-9 (MMP-9)[1]. Topoisomerase I/II inhibitor 2 (0–20 μM; 48 hours) stops the cell cycle at the G2/M phase, which prevents cells from proliferating[1]. In a concentration-dependent manner, topoisomerase I/II inhibitor 2 (3.5-20 μM; 48 hours) can damage mitochondrial function and cause cell apoptosis[1].
|
| Cell Assay |
Cell Proliferation Assay
Cell Types: LM9, HuH7, SK-hep-1, HepG2, HT-29, HCT-116, RKO, SW480, MCF-7, MDA-B-231, HGC-27, SGC-7901, BGC-823, A549, U251, HL-60, LO2[1] Tested Tested Concentrations: 0-150 μM Incubation Duration: 72 hrs (hours) Experimental Results: Displayed favorable anti-proliferative activity and had better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9). Western Blot Analysis Cell Types: LM9 and HuH7 cells[1] Tested Tested Concentrations: 0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7 Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited the expression of MMP-9. Cell Cycle Analysis Cell Types: LM9 and HuH7 cells[1] Tested Tested Concentrations: 0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7 Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited cells proliferation by blocking cell cycle at the G2/M phase. Apoptosis Analysis Cell Types: LM9 and HuH7 cells[1] Tested Tested Concentrations: 3.5, 7, 14 μM in LM9; 5, 10, 20 μM in HuH7 Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis in a dose-dependent manner. |
| References |
[1]. Deng X, et al. Design, synthesis and anti-hepatocellular carcinoma activity of 3-arylisoquinoline alkaloids. Eur J Med Chem. 2022;228:113985.
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| CAS # |
2770804-58-3
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|---|---|
| Appearance |
Typically exists as solid at room temperature
|
| 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)
|
| 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.) |
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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