| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Rubitecan (RFS-2000), a semisynthetic camptothecin analog, is an orally bioactive topoisomerase I inhibitor antitumor and antiviral activity. It inhibits DNA and RNA synthesis in dividing cells, induces protein-linked DNA single-strand breaks, and binds to topoisomerase I. prevents reversible single-strand DNA breaks from being repaired as well.
| Targets |
Topoisomerase I
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|---|---|
| ln Vitro |
Rubitecan (RFS 2000) suppresses CCL4, U-CH1, and U-CH2 cells with IC50 values of 7.7 µM, 0.83, and 0.32 µM, respectively[4].
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| References |
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| Additional Infomation |
Rubitecan is a pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin. It has a role as an antineoplastic agent, an EC 5.99.1.2 (DNA topoisomerase) inhibitor and a prodrug. It is a pyranoindolizinoquinoline, a C-nitro compound, a semisynthetic derivative, a tertiary alcohol and a delta-lactone.
Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks. (NCI04) Drug Indication Investigated for use/treatment in pancreatic cancer, leukemia (unspecified), melanoma, ovarian cancer, and cancer/tumors (unspecified). Mechanism of Action Rubitecan prevents DNA from unwinding during replication via DNA topoisomerase 1, therefore interfering with tumor growth. |
| Molecular Formula |
C20H15N3O6
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|---|---|
| Molecular Weight |
393.35
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| Exact Mass |
393.096
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| Elemental Analysis |
C, 61.07; H, 3.84; N, 10.68; O, 24.40
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| CAS # |
91421-42-0
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| PubChem CID |
472335
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
816.3±65.0 °C at 760 mmHg
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| Melting Point |
182-186ºC
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| Flash Point |
447.5±34.3 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.762
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| LogP |
1.38
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
29
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| Complexity |
861
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1C2COC([C@](C=2C=C2C3N=C4C=CC=C(C4=CC=3CN12)[N+](=O)[O-])(O)CC)=O
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| InChi Key |
VHXNKPBCCMUMSW-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C20H15N3O6/c1-2-20(26)13-7-16-17-10(8-22(16)18(24)12(13)9-29-19(20)25)6-11-14(21-17)4-3-5-15(11)23(27)28/h3-7,26H,2,8-9H2,1H3/t20-/m0/s1
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| Chemical Name |
(19S)-19-ethyl-19-hydroxy-8-nitro-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
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| Synonyms |
9-nitro-camptothecin; RFS-2000; RFS2000; RFS 2000; 9NC; nitrocamptothecin; 9-nitro-CPT; trade names: Camptogen; Orathecin
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| 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)
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| Solubility (In Vitro) |
DMSO: 58~62.5 mg/mL (147.5~158.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5423 mL | 12.7113 mL | 25.4227 mL | |
| 5 mM | 0.5085 mL | 2.5423 mL | 5.0845 mL | |
| 10 mM | 0.2542 mL | 1.2711 mL | 2.5423 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00005872 | Completed | Drug: rubitecan | Lung Cancer | Astex Pharmaceuticals, Inc. | May 1999 | Phase 2 |
| NCT00006230 | Completed | Drug: rubitecan | Ovarian Cancer | European Organisation for Research and Treatment of Cancer - EORTC |
May 2000 | Phase 2 |
| NCT00006082 | Completed | Drug: rubitecan | Lung Cancer | European Organisation for Research and Treatment of Cancer - EORTC |
May 2000 | Phase 2 |
| NCT00006026 | Completed | Drug: rubitecan | Bladder Cancer Urethral Cancer |
European Organisation for Research and Treatment of Cancer - EORTC |
May 2000 | Phase 2 |
| NCT00005826 | Completed | Drug: rubitecan | Brain and Central Nervous System Tumors |
European Organisation for Research and Treatment of Cancer - EORTC |
March 2000 | Phase 2 |
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