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MedKoo Biosciences/KP372-1/401520/500mg

KP372-1isasyntheticsmallmoleculeAKTinhibitor.KP372-1isconsistedoftwoisomers:KP372-1AandKP372-1B.KP372-1showedactivitiestoblocksignallingdownstreamofAktinthyroidtumourcells,leADIngtoinhibitionofcellproliferationandincreasedapoptosis.KP372-1hasalsobeenshowntosuppresscellproliferationandinduceapoptosisingliobastoma.

MedKooCat#:401520
Name:KP372-1
CAS#:329710-24-9
ChemicalFormula:C10H4N6O
ExactMass:224.04466
MolecularWeight:224.17836
ElementalAnalysis:C,53.58;H,1.80;N,37.49;O,7.14


Synonym:KP3721,KP3721,KP-3721

IUPAC/ChemicalName:KP372-1A:10H-indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one

InChiKey:SSNMLKNJEUSPDY-UHFFFAOYSA-N

InChiCode:InChI=1S/C10H4N6O/c17-9-6-4-2-1-3-5(6)7-8(9)11-10-12-14-15-16(10)13-7/h1-4H

SMILESCode:O=C(C1=NC2=NN=NN2N=C13)C4=C3C=CC=C4


TechnicalData

Appearance:
Solidpowder

Purity:
>98%

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

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

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>5yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

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

HarmonizedSystemCode:
293490


AdditionalInformation

 
 
 
 


References

1:LiuB,WuJM,LiJ,LiuJJ,LiWW,LiCY,XuHL,BaoJK.PolygonatumcyrtonemalectininducesmurinefibrosarcomaL929cellapoptosisandautophagyviablockingRas-RafandPI3K-Aktsignalingpathways.Biochimie.2010Dec;92(12):1934-8.Epub2010Aug14.PubMedPMID:20713122.

2:ShaoH,YiXM,WellsA.EpidermalgrowthfactorprotectsfibroblastsfromapoptosisviaPI3kinaseandRacsignalingpathways.WoundRepairRegen.2008Jul-Aug;16(4):551-8.PubMedPMID:18638274;PubMedCentralPMCID:PMC2547354.

3:XiRG,HuangJ,LiD,WangXB,WuLJ.RolesofPI3-K/Aktpathwaysinnanoparticlerealgarpowders-inducedapoptosisinU937cells.ActaPharmacolSin.2008Mar;29(3):355-63.PubMedPMID:18298901.

4:LiD,CuiQ,ChenSG,WuLJ,TashiroS,OnoderaS,IkejimaT.Inactivationofrasandchangesofmitochondrialmembranepotentialcontributetooridonin-inducedautophagyina431cells.JPharmacolSci.2007Sep;105(1):22-33.PubMedPMID:17895587.

5:ZengZ,SamudioIJ,ZhangW,EstrovZ,PelicanoH,HarrisD,FrolovaO,HailNJr,ChenW,KornblauSM,HuangP,LuY,MillsGB,AndreeffM,KonoplevaM.SimultaneousinhibitionofPDK1/AKTandFms-liketyrosinekinase3signalingbyasmall-moleculeKP372-1inducesmitochondrialdysfunctionandapoptosisinacutemyelogenousleukemia.CancerRes.2006Apr1;66(7):3737-46.PubMedPMID:16585200.

6:KoulD,ShenR,BerghS,ShengX,ShishodiaS,LafortuneTA,LuY,deGrootJF,MillsGB,YungWK.InhibitionofAktsurvivalpathwaybyasmall-moleculeinhibitorinhumanglioblastoma.MolCancerTher.2006Mar;5(3):637-44.PubMedPMID:16546978.

7:MandalM,YounesM,SwanEA,JasserSA,DoanD,YigitbasiO,McMurpheyA,LudwickJ,El-NaggarAK,BucanaC,MillsGB,MyersJN.TheAktinhibitorKP372-1inhibitsproliferationandinducesapoptosisandanoikisinsquamouscellcarcinomaoftheheadandneck.OralOncol.2006Apr;42(4):430-9.Epub2006Jan27.PubMedPMID:16442835;PubMedCentralPMCID:PMC1414640.

8:MandalM,KimS,YounesMN,JasserSA,El-NaggarAK,MillsGB,MyersJN.TheAktinhibitorKP372-1suppressesAktactivityandcellproliferationandinducesapoptosisinthyroidcancercells.BrJCancer.2005May23;92(10):1899-905.PubMedPMID:15870708;PubMedCentralPMCID:PMC2361761.

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