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商品描述
- PX-866,aderivativeofwortmannin,potentlyinhibitedpurifiedphosphoinositide(PtdIns)-3-kinase(IC50=0.1nM)andPtdIns-3-kinasesignaling(IC50=20nM)asassessedbyphospho-Ser473-AktlevelsinHT-29coloncancercells.PX-866showedantitumoractivityinvivoagainsts.c.A-549humanlungcancerxenograftsandOvCar-3humanovariancancerinimmunodeficientmice.PX-866alsoenhancedtheantitumoractivityofcisplatinagainstA-549xenograftsandrADIationtreatmentagainstOvCar-3xenografts.Ihle,N.T.,etal."MolecularpharmacologyandantitumoractivityofPX-866,anovelinhibitorofphosphoinositide-3-kinasesignaling."Mol.CancerTher.3:763-772(2004).
- PX-866appearstoinhibittumorgrowthbyblockingthephosphatidylinositol3-kinase(PI3K)pathwayandcellmotility.Howes,A.L.,etal."Thephosphatidylinositol3-kinaseinhibitor,PX-866,isapotentinhibitorofcancercellmotilityandgrowthinthree-dimensionalcultures."Mol.CancerTher.6:2505-2514(2007).
- HyperglycemiaisasideeffectofPX-866treatment.Combinationtreatmentofperoxisomeproliferator-activatedreceptorγagoNISTpioglitazonewithPX-688canovercometheincreaseinbloodglucosewithoutaffectingantitumoractivitycausedbyPX-866.Ihle,N.T.,etal."Peroxisomeproliferator-activatedreceptorgammaagonistpioglitazonepreventsthehyperglycemiacausedbyphosphatidylinositol3-kinasepathwayinhibitionbyPX-866withoutaffectingantitumoractivity."Mol.CancerTher.8:94-100(2009).
- PX-866isaPI3-Kinhibitorwithselectivityforp110α.ItenhancedtheantitumoractivityofgefitinibagainstA-549non-smallcelllungcancer(NSCLC)xenografts,givingcompletetumorgrowthcontrolduringtheearlystagesoftreatment.Ihle,N.T.,etal."Thephosphatidylinositol-3-kinaseinhibitorPX-866overcomesresistancetotheepidermalgrowthfactorreceptorinhibitorgefitinibinA-549humannon-smallcelllungcancerxenografts."Mol.CancerTher.4:1349-1357(2005).
- STRUCTURENOTE:ChemicalAbstractsServicedefinesPX-866ashavingthe"E"configurationfortheenaminedoublebondatthelowerleftcornerofthestructure.Atleastoneothervendor"sstructureforPX-866hastheincorrect"Z"configurationforthatdoublebond.
- Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
- ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanadianpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
- Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.
C29H35NO8
[502632-66-8]