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Topovale
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Catalog No. T9088Cas No. 500214-53-9
Alias Topoval, ARC-111, ARC111, ARC 111
Topovale (ARC111) is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.
Topovale
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Purity: 99.94%
Catalog No. T9088Alias Topoval, ARC-111, ARC111, ARC 111Cas No. 500214-53-9
Topovale (ARC111) is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $88 | In Stock | In Stock | |
| 5 mg | $179 | In Stock | In Stock | |
| 10 mg | $255 | In Stock | In Stock | |
| 25 mg | $460 | In Stock | In Stock | |
| 50 mg | $676 | In Stock | In Stock | |
| 100 mg | $962 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.94%
Appearance:Solid
Color:White
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Product Introduction
Topovale AI Summary
Topovale demonstrates significant bioactivity, particularly in its cytotoxic effects against various cancer cell lines and its inhibition of DNA topoisomerase I activity. It has potently inhibited the growth of cancer cell lines such as human lymphoblast RPMI 8402 and mouse P388, with IC50 values typically ranging from as low as 1.0 nM to 900.0 nM in camptothecin-resistant lines. Notably, in topoisomerase I-mediated DNA cleavage assays, Topovale exhibits an efficacy comparable to topotecan, with a relative concentration (REC) value of 0.5. The compound remains effective against multi-drug resistant and camptothecin-resistant variants, demonstrating its robustness. Additionally, it has shown significant antitumor activity in in vivo studies in NCR-nude-nude mice with MDA-MB-435 xenografts, administering both orally and intraperitoneally. These characteristics suggest that Topovale holds promise as a potent anti-cancer agent through its dual mechanisms of action: topoisomerase inhibition and strong cytotoxic effects on a wide array of cancer cells..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Topovale (ARC111) is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells. |
| Synonyms | Topoval, ARC-111, ARC111, ARC 111 |
| Molecular Weight | 421.45 |
| Formula | C23H23N3O5 |
| Cas No. | 500214-53-9 |
| Smiles | C(CN(C)C)N1C2=C(C=3C(C1=O)=CC(OC)=C(OC)C3)C=NC=4C2=CC5=C(C4)OCO5 |
| Relative Density. | 1.325 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: Insoluble  |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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