Eniluracil
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H201250

CAS#: 59989-18-3

Description: Eniluracil, also known as GW776 and GW776C85, is an orally active and irreversible inhibitor of dihydropyrimidine dehydrogenase. 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. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).


Chemical Structure

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Eniluracil
CAS# 59989-18-3

Theoretical Analysis

Hodoodo Cat#: H201250
Name: Eniluracil
CAS#: 59989-18-3
Chemical Formula: C6H4N2O2
Exact Mass: 136.03
Molecular Weight: 136.110
Elemental Analysis: C, 52.95; H, 2.96; N, 20.58; O, 23.51

Price and Availability

Size Price Availability Quantity
100mg USD 250 2 weeks
200mg USD 450 2 weeks
500mg USD 900 2 weeks
1g USD 1450 2 weeks
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Synonym: 776C85; DH300004; GW776; GW-776; GW 776; GW-776C85; GW 776C85; GW776C85; NSC 687296; 5-ethynyluracil; ethynyluracil.

IUPAC/Chemical Name: 5-ethynylpyrimidine-2,4(1H,3H)-dione.

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)

SMILES Code: O=C1NC(C(C#C)=CN1)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Eniluracil plus 5‑FU was previously being developed by GlaxoSmithKline (GSK). Although the therapy was successful in Phase I and Phase II clinical trials, it tended to produce less antitumor activity than the control therapy in two Phase III trials. Development was subsequently stopped. Since then, Adherex has learned that with the dose and schedule used in the previous GSK Phase III trials may not have been optimal. Preclinical studies have shown that when eniluracil is present in high ratios to 5‑FU, it decreases the antitumor activity. In the Phase III trials, the eniluracil:5‑FU ratio was 10:1. see: http://adherex.com/product-candidate/eniluracil-clinical-development/   Eniluracil is a potent inactivator of dihydropyrimidine dehydrogenase (uracil reductase), the enzyme that rapidly catabolizes 5-fluorouracil (5-FU). Although eniluracil in combination with 5-FU was promising in phase I and II studies, in 2 multicenter phase III colorectal cancer studies, eniluracil dosed in a 10-to-1 ratio to 5-FU produced less antitumor benefit than the std. regimen of 5-FU/leucovorin without eniluracil.  Clinical Colorectal Cancer (2010), 9(1), 52-54.    

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 136.11 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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