| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
Orally accessible IUdR (5-iodo-2'-deoxyuridine) prodrug is ropidoxuridine. At therapeutically meaningful doses, ropidoxuridine and alisertib show significant synergism [1].
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|---|---|
| ln Vivo |
Alisertib (30 mg/kg/day) and ropidoxuridine (750 mg/kg/day) demonstrated a significant synergistic effect in orthotopic tumor models [1].
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| References | |
| Additional Infomation |
Ropidoxuridine is a novel, orally available, thymidine analogue and prodrug for IUdR, which demonstrated a survival advantage in Phase II studies in anaplastic astrocytoma, a type of brain tumor.
Ropidoxuridine is an orally available 5-substituted 2-pyrimidinone-2'-deoxyribonucleoside analogue and prodrug of 5-iododeoxyuridine (IUdR), an iodinated analogue of deoxyuridine, with radiosensitizing activity. Upon oral administration, ropidoxuridine (IPdR) is efficiently converted to idoxuridine (IUdR) by a hepatic aldehyde oxidase. In turn, IUdR is incorporated into DNA during replication, thereby sensitizing cells to ionizing radiation by increasing DNA strand breaks. Compared to IUdR, ropidoxuridine is associated with a lower toxicity profile and improved anti-tumor activity. Drug Indication Investigated for use/treatment in cancer/tumors (unspecified). |
| Molecular Formula |
C9H11IN2O4
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|---|---|
| Molecular Weight |
338.1
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| Exact Mass |
337.976
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| CAS # |
93265-81-7
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| PubChem CID |
9840777
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
2.22g/cm3
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| Boiling Point |
478.6ºC at 760mmHg
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| Flash Point |
243.3ºC
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| Index of Refraction |
1.759
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
357
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1[C@@H]([C@H](O[C@H]1N2C=C(C=NC2=O)I)CO)O
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| InChi Key |
XIJXHOVKJAXCGJ-XLPZGREQSA-N
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| InChi Code |
InChI=1S/C9H11IN2O4/c10-5-2-11-9(15)12(3-5)8-1-6(14)7(4-13)16-8/h2-3,6-8,13-14H,1,4H2/t6-,7+,8+/m0/s1
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| Chemical Name |
1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidin-2-one
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| Synonyms |
5-Iodo-2-pyrimidinone-2-deoxyribose IPdR D08992 Ropidoxuridine
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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 : ~250 mg/mL (~739.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.9577 mL | 14.7885 mL | 29.5770 mL | |
| 5 mM | 0.5915 mL | 2.9577 mL | 5.9154 mL | |
| 10 mM | 0.2958 mL | 1.4789 mL | 2.9577 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 |
| NCT06359379 | NOT YET RECRUITING | Drug: Ropidoxuridine | Glioblastoma, IDH-wildtype | Shuttle Pharmaceuticals, Inc. | 2024-06 | Phase 2 |
| NCT02993146 | ACTIVE, NOT RECRUITINGWITH RESULTS | Other: Laboratory Biomarker Analysis Other: Pharmacological Study Other: Quality-of-Life Assessment |
Hematopoietic and Lymphoid Cell Neoplasm Malignant Solid Neoplasm Metastatic Malignant Neoplasm in the Brain |
National Cancer Institute (NCI) | 2017-05-08 | Phase 1 |
| NCT02381561 | ACTIVE, NOT RECRUITING | Radiation: Intensity-Modulated Radiation Therapy Other: Laboratory Biomarker Analysis Other: Pharmacological Study Drug: Ropidoxuridine |
Advanced Bile Duct Carcinoma Stage II Esophageal Cancer AJCC v7 Stage II Pancreatic Cancer AJCC v6 and v7 Stage IIA Esophageal Cancer AJCC v7 |
National Cancer Institute (NCI) | 2016-02-01 | Phase 1 |
| NCT04406857 | TERMINATEDWITH RESULTS | Drug: Capecitabine Radiation: Radiation Therapy Drug: Ropidoxuridine |
Locally Advanced Rectal Carcinoma Rectal Adenocarcinoma Stage II Rectal Cancer AJCC v8 Stage III Rectal Cancer AJCC v8 |
National Cancer Institute (NCI) | 2021-03-17 | Phase 1 |
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