Top1 inhibitor 1
Based on 1 Customer Validation
Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.67%
- No. CAS: 2302772-05-8
- Fòrmula: C24H22N6O2
- Peso molecular:426.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Camptothecins |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
2.34 μM
Compound: 28
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Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| HEK293 | IC50 |
8.34 μM
Compound: 1
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hr by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hr by MTT assay
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[PMID: 32682183] |
| HEK293 | IC50 |
8.34 μM
Compound: 28
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| HeLa | IC50 |
2.61 μM
Compound: 28
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| MCF7 | IC50 |
2.74 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hr by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hr by MTT assay
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[PMID: 32682183] |
| MCF7 | IC50 |
2.74 μM
Compound: 28
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| MCF7 | IC50 |
2.74 μM
Compound: 28
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Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
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[PMID: 30897325] |
| MEF | IC50 |
1.02 μM
Compound: 28
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Cytotoxicity against TDP1-deficient MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against TDP1-deficient MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| MEF | IC50 |
2.91 μM
Compound: 28
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Cytotoxicity against TDP1-positive MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against TDP1-positive MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30897325] |
| Sf9 | IC50 |
0.029 μM
Compound: 28
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Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
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[PMID: 30897325] |
Top1 inhibitor 1 reveals cytotoxicity in cancerous cells including MCF7 (IC50: 2.74 µM), HeLa (IC50: 2.61 µM), HCT116 (IC50: 2.34 µM), NIH: OVCAR-3 (IC50: 2.35 µM) cells compared to the non-cancerous cells like HEK293 (IC50: 8.34 µM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2302772-05-8
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Appearance Solid
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Peso molecular 426.47
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Fòrmula C24H22N6O2
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Color Off-white to light yellow
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SMILES
COC(C=C1)=CC=C1C2=CC=C(N=CC(C3=NN=CO3)=C4NCCCN5C=NC=C5)C4=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 6.67 mg/mL (15.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.67 mg/mL (1.57 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.57 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | 58.6208 mL |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | 11.7242 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9081 mL |
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