产品资料

MedKoo Biosciences/Eniluracil/201250/25mg

Eniluracil,alsoknownasGW776andGW776C85,isanorallyactiveandirreversIBLeinhibitorofdihydropyrimidinedehydrogenase.Eniluracilinhibitsdihydropyrimidinedehydrogenase,therate-limitingenzymethatcatabolizesandinactivates5-fluorouracil(5-FU)intheliver.Co-admiNISTrationofethynyluracilpermitstheoraladministrationof5-FU.Checkforactiveclinicaltrialsorclosedclinicaltrialsusingthisagent.(NCIThesaurus).

MedKooCat#:201250
Name:Eniluracil
CAS#:59989-18-3
ChemicalFormula:C6H4N2O2
ExactMass:136.02728
MolecularWeight:136.11
ElementalAnalysis:C,52.95;H,2.96;N,20.58;O,23.51

Synonym:776C85;DH300004;GW776;GW-776;GW776;GW-776C85;GW776C85;GW776C85;NSC687296;5-ethynyluracil;ethynyluracil.

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

InChiKey:JOZGNYDSEBIJDH-UHFFFAOYSA-N

InChiCode:InChI=1S/C6H4N2O2/c1-2-4-3-7-6(10)8-5(4)9/h1,3H,(H2,7,8,9,10)

SMILESCode:O=C1NC(C(C#C)=CN1)=O

TechnicalData

Appearance:

Solidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:

Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:

Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:

SolubleinDMSO,notinwater

ShelfLife:

>2yearsifstoredproperly

DrugFormulation:

ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:

0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:

293490

AdditionalInformation

Eniluracilplus5‑FUwaspreviouslybeingdevelopedbyGlaxoSmithKline(GSK).AlthoughthetherapywassuccessfulinPhaseIandPhaseIIclinicaltrials,ittendedtoproducelessantitumoractivitythanthecontroltherapyintwoPhaseIIItrials.Developmentwassubsequentlystopped.Sincethen,AdherexhaslearnedthatwiththedoseandscheduleusedinthepreviousGSKPhaseIIItrialsmaynothavebeenoptimal.Preclinicalstudieshaveshownthatwheneniluracilispresentinhighratiosto5‑FU,itdecreasestheantitumoractivity.InthePhaseIIItrials,theeniluracil:5‑FUratiowas10:1.see:http://adherex.com/product-candidate/eniluracil-clinical-development/

Eniluracilisapotentinactivatorofdihydropyrimidinedehydrogenase(uracilreductase),theenzymethatrapidlycatabolizes5-fluorouracil(5-FU).Althougheniluracilincombinationwith5-FUwaspromisinginphaseIandIIstudies,in2multicenterphaseIIIcolorectalcancerstudies,eniluracildosedina10-to-1ratioto5-FUproducedlessantitumorbenefitthanthestd.regimenof5-FU/leucovorinwithouteniluracil. ClinicalColorectalCancer(2010),9(1),52-54.

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MedKoo Biosciences/Eniluracil/201250/25mg

TechnicalData

AdditionalInformation

References