| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Eniluracil (also known as 5-Ethynyluracil; GW776C85) is a novel and potent uracil analog and also a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), which increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
| ln Vivo |
Rats treated with Eniluracil (5-ethynyluracil) at a dose of 1 mg/kg intraperitoneally once a day for three days experience a significant improvement in FUra (5-fluorouracil) response to treatment, without any side effects or inherent antitumor activity[1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Female Fischer 344/HSD rats (6 to 7 weeks old; 150-200 g) [1].
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 3 days (1 hour before FUra (5-fluorouracil) and an additional 2 days after FUra treatment) Experimental Results: When combined with 3.5 mg/kg FUra, tumor Complete regression persisted for at least 90 days after treatment, but 35 mg/kg FUra alone produced a partial response in 75% of treated animals (tumor regrowth in all of these animals). |
| References |
|
| Additional Infomation |
Eniluracil is a pyrimidone.
Eniluracil, which was previously under development by GlaxoSmithKline (GSK), is being developed by Adherex to enhance the therapeutic value and effectiveness of 5-fluorouracil (5-FU), one of the world’s most widely-used oncology agents. 5-FU is widely used in the U.S. and is often first or second line therapy for a variety of cancers including colorectal, breast, gastric, head and neck, ovarian and basal cell cancer of the skin. Eniluracil could improve 5-FU by increasing its effectiveness, reducing its side effects and/or making it orally available. Eniluracil has received Orphan Drug status from the FDA for the treatment of hepatocellular cancer in combination with fluoropyrimidines (including 5-FU). Eniluracil is an orally-active fluoropyrimidine analogue. Eniluracil inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme that catabolizes and inactivates 5-fluorouracil (5-FU) in the liver. Co-administration of ethynyluracil permits the oral administration of 5-FU. Drug Indication For the treatment of cancer in combination with 5-fluorouracil. Mechanism of Action Normally, 5-FU is rapidly broken down in the body by an enzyme known as dihydropyrimidine dehydrogenase (DPD). Eniluracil irreversibly inhibits DPD, thereby substantially slowing the breakdown of 5-FU and prolonging exposure of the tumor cells to the drug. |
| Molecular Formula |
C6H4N2O2
|
|---|---|
| Molecular Weight |
136.1082
|
| Exact Mass |
136.027
|
| CAS # |
59989-18-3
|
| PubChem CID |
43157
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.39g/cm3
|
| Melting Point |
320 °C(dec.)
|
| Index of Refraction |
1.589
|
| LogP |
-0.7
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
10
|
| Complexity |
269
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C(C#C[H])=C([H])N([H])C(N1[H])=O
|
| InChi Key |
JOZGNYDSEBIJDH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C6H4N2O2/c1-2-4-3-7-6(10)8-5(4)9/h1,3H,(H2,7,8,9,10)
|
| Chemical Name |
5-ethynyl-1H-pyrimidine-2,4-dione
|
| Synonyms |
5-Ethynyluracil; GW-776C85; GW 776C85; GW776C85
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~16.67 mg/mL (~122.47 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (15.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (15.28 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (15.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.3470 mL | 36.7350 mL | 73.4700 mL | |
| 5 mM | 1.4694 mL | 7.3470 mL | 14.6940 mL | |
| 10 mM | 0.7347 mL | 3.6735 mL | 7.3470 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA