Eniluracil
Based on 1 publication(s) in Google Scholar
Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil). Eniluracil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Purity: 99.87%
- CAS No.: 59989-18-3
- 화학식: C6H4N2O2
- 분자량:136.11
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Eniluracil
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Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Fischer 344/HSD rats (6 to 7-week-old; 150-200 g)[1].
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; single daily for 3 days (l h before FUra (5-fluorouracil) and for an additional 2 days after FUra therapy)
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Result:Produced complete tumor regression that was sustained for at least 90 days posttherapy when combined with 3.5 mg/kg FUra, however, 35 mg/kg FUra alone produced partial responses in 75% of the treated animals ( the tumors regrew in all of these animals).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 59989-18-3
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Appearance Solid
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분자량 136.11
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화학식 C6H4N2O2
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Color White to yellow
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SMILES
O=C(N1)NC=C(C#C)C1=O
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Synonyms
5-Ethynyluracil; GW776C85
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 5.56 mg/mL (40.85 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 0.56 mg/mL (4.11 mM); Clear solution
This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.56 mg/mL (4.11 mM); Clear solution
This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Cao S, et al. 5-Ethynyluracil (776C85): modulation of 5-fluorouracil efficacy and therapeutic index in rats bearing advanced colorectal carcinoma. Cancer Res. 1994 Mar 15;54(6):1507-10. [Content Brief]
[2]. Schilsky RL, et al. Eniluracil: an irreversible inhibitor of dihydropyrimidine dehydrogenase. Expert Opin Investig Drugs. 2000 Jul;9(7):1635-49. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 7.3470 mL | 36.7350 mL | 73.4700 mL | 183.6750 mL |
| 5 mM | 1.4694 mL | 7.3470 mL | 14.6940 mL | 36.7350 mL | |
| 10 mM | 0.7347 mL | 3.6735 mL | 7.3470 mL | 18.3675 mL | |
| 15 mM | 0.4898 mL | 2.4490 mL | 4.8980 mL | 12.2450 mL | |
| 20 mM | 0.3673 mL | 1.8367 mL | 3.6735 mL | 9.1837 mL | |
| 25 mM | 0.2939 mL | 1.4694 mL | 2.9388 mL | 7.3470 mL | |
| 30 mM | 0.2449 mL | 1.2245 mL | 2.4490 mL | 6.1225 mL | |
| 40 mM | 0.1837 mL | 0.9184 mL | 1.8367 mL | 4.5919 mL |
Eniluracil Related Classifications
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