产品资料

MedKoo Biosciences/BAL27862/205822/500mg

BAL27862isaanovelsyntheticpotentinhibitoroftubulinpolymerizationthatinducescancercelldeath.BAL27862isanovelmicrotubule-destABIlizingdrugthatiscurrentlyundergoingphaseIclinicalevaluationastheprodrugBAL101553.BAL27862elicitsauniquemicrotubule(MT)phenotype,distinctfrompaclitaxel,vinblastineandcolchicine,hasbroadinvitroanti-proliferativeactivityagainstadiverserangeofhumantumorlines(lownMIC50s)andinducessignificantantitumorresponsesinarange

MedKooCat#:205822
Name:BAL27862
CAS#:798577-91-0
ChemicalFormula:C20H17N7O2
ExactMass:387.14437
MolecularWeight:387.39
ElementalAnalysis:C,62.01;H,4.42;N,25.31;O,8.26

Synonym:BAL27862;BAL-27862;BAL27862

IUPAC/ChemicalName:3-((4-(1-(2-(4-aminophenyl)-2-oxoethyl)-1H-benzo[d]imidazol-2-yl)-1,2,5-oxADIazol-3-yl)amino)propanenitrile

InChiKey:LSFOZQQVTWFMNS-UHFFFAOYSA-N

InChiCode:InChI=1S/C20H17N7O2/c21-10-3-11-23-19-18(25-29-26-19)20-24-15-4-1-2-5-16(15)27(20)12-17(28)13-6-8-14(22)9-7-13/h1-2,4-9H,3,11-12,22H2,(H,23,26)

SMILESCode:N#CCCNC1=NON=C1C2=NC3=CC=CC=C3N2CC(C4=CC=C(N)C=C4)=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

BAL27862isanovelMTAthattriggersapoptosisincancercells.Invitro,BAL27862destabilizesmicrotubulestoproduceamicrotubulephenotypedistinctfromthatobservedwithotherMTAs,andretainsitsantiproliferativeactivityagainstP-gpoverexpressingtumorcells.BAL27862,whenadmiNISTeredintravenouslyororally,inducessignificantantitumorresponsesinarangeofanimalmodelsofhumancancer,includingtumorsrefractorytoconventionaltreatments.BAL27862overcomesP-gpoverexpression-mediatedresistance,anddemonstratethatBcl-2statusandtubulinmodificationsdonotnecessarilyaffectitsantitumoractivity.AnalysisofMDsshowsthatBAL27862elicitedeffectsconsistentwithitsdestabilizingactivity;suppressionofMDswas2-foldlowerthanobservedwithPTX.Strikingly,BAL27862displayedauniquemicrotubuleseveringactivity.Conclusions:Besidesitsmicrotubule-targetingactivity,BAL27862displaysuniquefeaturesinitsmechanismofactionthatmakeitapromisingcompoundforclinicalinvestigation. (source:JClinOncol28,2010(suppl;abstre13589)

References

1:ProtaAE,DanelF,BachmannF,BargstenK,BueyRM,PohlmannJ,ReineltS,LaneH,SteinmetzMO.Thenovelmicrotubule-destabilizingdrugBAL27862bindsto thecolchicinesiteoftubulinwithdistincteffectsonmicrotubuleorganization.JMolBiol.2014Apr17;426(8):1848-60.doi:10.1016/j.jmb.2014.02.005.Epub2014Feb11.PubMedPMID:24530796.

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MedKoo Biosciences/BAL27862/205822/500mg

TechnicalData

AdditionalInformation

References