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Rubitecan

Name: Rubitecan
Brand: TargetMol
SKU: T5853
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5853Cas No. 91421-42-0

Alias RFS 2000, 9-Nitrocamptothecin

Rubitecan (9-Nitrocamptothecin) is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner.Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties.

Rubitecan

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Purity: 97.54%

Catalog No. T5853Alias RFS 2000, 9-NitrocamptothecinCas No. 91421-42-0

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$40	In Stock	In Stock
25 mg	$89	In Stock	In Stock
50 mg	$129	-	In Stock
100 mg	$193	-	In Stock
1 mL x 10 mM (in DMSO)	$30	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.54%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Rubitecan AI Summary

Rubitecan is a lactone compound that exhibits a wide range of biological activities. It has demonstrated significant antitumor effects against P-338 leukemia in mice, extending the survival time of treated animals to 348% of control animals and achieving 5 cures within an active dose range of 2.5 to 20 mg/kg, with a toxic dose of 40 mg/kg. In lactone metabolism studies, Rubitecan causes a rapid decrease in lactone levels in human and mouse plasma, reaching 0% in humans and 18-30% in mice within a few hours. The compound shows potency in inhibiting ROR gamma transcriptional activity (89.1 nM to 631.0 nM), activities against the malarial parasite plastid, and inhibition of USP1/UAF1 (63095.7 nM). It induces apoptosis in human Caco2 cells with IC50 values between 112.0 nM and 479.0 nM and is active in assays involving Schwann cells and colon adenocarcinoma cells. Rubitecan also inhibits various human multidrug resistance-associated proteins (MRP2, MRP3, and MRP4) with varying IC50 values and has weak activity against human BSEP. While showing no significant antifungal or antibacterial effects, Rubitecan exhibits antiviral activity against SARS-CoV-2. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 µM, showing a reduction in cytotoxicity by 37.5% in Caco-2 cells but with relatively high IC50 values indicating weaker potency. Additionally, Rubitecan has limited binding affinity towards various human receptors and enzymes, with non-significant activity levels in most cases. It exhibits some antagonistic activity at human TBXA2R and weak inhibitory effects on human ACHE, but these are not prominent compared to its other bioactivities..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Rubitecan (9-Nitrocamptothecin) is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner.Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties.
Synonyms	RFS 2000, 9-Nitrocamptothecin

Chemical Properties

Molecular Weight	393.35
Formula	C₂₀H₁₅N₃O₆
Cas No.	91421-42-0
Smiles	CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cccc([N+]([O-])=O)c4cc3Cn1c2=O
Relative Density.	1.63g/cm3

Storage & Solubility Information

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: 50 mg/mL (127.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5423 mL	12.7113 mL	25.4227 mL	127.1133 mL
5 mM	0.5085 mL	2.5423 mL	5.0845 mL	25.4227 mL
10 mM	0.2542 mL	1.2711 mL	2.5423 mL	12.7113 mL
20 mM	0.1271 mL	0.6356 mL	1.2711 mL	6.3557 mL
50 mM	0.0508 mL	0.2542 mL	0.5085 mL	2.5423 mL
100 mM	0.0254 mL	0.1271 mL	0.2542 mL	1.2711 mL

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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