Rubitecan
Based on 1 Customer Validation
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.41%
- No. CAS: 91421-42-0
- Fòrmula: C20H15N3O6
- Peso molecular:393.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
Topoisomerase I[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.138 μM
Compound: Rubitecan
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Cytotoxicity against human A375 cells after 24 hrs by MTT assay
Cytotoxicity against human A375 cells after 24 hrs by MTT assay
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[PMID: 24980118] |
| Caco-2 | IC50 |
0.112 μM
Compound: Rubitecan
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Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay
Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay
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[PMID: 24980118] |
| HeLa | IC50 |
0.343 μM
Compound: Rubitecan
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Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
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[PMID: 24980118] |
| Jurkat | IC50 |
0.128 μM
Compound: Rubitecan
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Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay
Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay
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[PMID: 24980118] |
| MDA-MB-231 | IC50 |
0.479 μM
Compound: Rubitecan
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Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
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[PMID: 24980118] |
In Vitro
Rubitecan (RFS 2000) inhibits U-CH1, U-CH2, and CCL4 cells with IC50s 0.32, 0.83, and 7.7 μM, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 91421-42-0
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Appearance Solid
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Peso molecular 393.35
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Fòrmula C20H15N3O6
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Color Light yellow to yellow
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SMILES
O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C([N+]([O-])=O)C=CC=C5N=C4C3=C2)=O
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Synonyms
RFS 2000; 9-Nitrocamptothecin
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Structure Classification
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Initial Source
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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 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : 62.5 mg/mL (158.89 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (5.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Protocolo
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureza y Documentación
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Ficha de datos (290 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Burris HA 3rd, et al. Phase II trial of oral rubitecan in previously treated pancreatic cancer patients. Oncologist. 2005 Mar;10(3):183-90. [Content Brief]
[2]. Rubitecan: 9-NC, 9-Nitro-20(S)-camptothecin, 9-nitro-camptothecin, 9-nitrocamptothecin, RFS 2000, RFS2000. Drugs R D. 2004;5(5):305-11. [Content Brief]
[3]. Rubitecan
[4]. Xia M, et al. Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther. 2013 Jul;14(7):638-47. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5423 mL | 12.7113 mL | 25.4227 mL | 63.5566 mL |
| 5 mM | 0.5085 mL | 2.5423 mL | 5.0845 mL | 12.7113 mL | |
| 10 mM | 0.2542 mL | 1.2711 mL | 2.5423 mL | 6.3557 mL | |
| 15 mM | 0.1695 mL | 0.8474 mL | 1.6948 mL | 4.2371 mL | |
| 20 mM | 0.1271 mL | 0.6356 mL | 1.2711 mL | 3.1778 mL | |
| 25 mM | 0.1017 mL | 0.5085 mL | 1.0169 mL | 2.5423 mL | |
| 30 mM | 0.0847 mL | 0.4237 mL | 0.8474 mL | 2.1186 mL | |
| 40 mM | 0.0636 mL | 0.3178 mL | 0.6356 mL | 1.5889 mL | |
| 50 mM | 0.0508 mL | 0.2542 mL | 0.5085 mL | 1.2711 mL | |
| 60 mM | 0.0424 mL | 0.2119 mL | 0.4237 mL | 1.0593 mL | |
| 80 mM | 0.0318 mL | 0.1589 mL | 0.3178 mL | 0.7945 mL | |
| 100 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6356 mL |
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