• Perifosine,alsoknownasKRX-0401,isanovelsyntheticalkylphospholipidandisanewkindofantitumoragentwhichtargetscellmembranesandblocksAktactivation.
• Thestructureofperifosineissimilartonaturally-occurringphospholipids.Perifosine(5µM)inhibitedthegrowthofPC-3prostatecarcinomacellsby50%in24hrandinducedcelldeathinvirtuallyallcellsby48hr.Kondapaka,S.B.,etal."Perifosine,anovelalkylphospholipid,inhibitsproteinkinaseBactivation."Mol.CancerTher.2:1093-1103(2003).
• Perifosineinhibitsthegrowthofvariantcells,withGI50valuesof1-10µMforK-562,SUDHL-7,HL-60,PC-3,Colo-205,andMESA-SA(CRL-1976)cells,11-30µMforMG-63(CRL-1427),H-3386,RD(CCL-136),HT-29,MDA-435,SW-620,CCRF-7,H-1355,SAJA-1(CRL-2098),andDU-145cells,and>30µMforMCF-7,Hos(CRL-1543),andLnCAPcells.Kondapaka,S.B.,etal."Perifosine,anovelalkylphospholipid,inhibitsproteinkinaseBactivation."Mol.CancerTher.2:1093-1103(2003).
• PerifosinereducesAktactivitybyinhibitingphosphorylationofAktatbothThr308andSer473.Kondapaka,S.B.,etal.Perifosine,anovelalkylphospholipid,inhibitsproteinkinaseBactivation."Mol.CancerTher.2:1093-1103(2003).
• Perifosineinhibitedthegrowthofbreast,ovarianandprostatecancersbyinducingapoptosis.PerifosineselectivelyblocksAKTrecruitmenttothemembraneanddown-regulatesthephosphorylationofAKTanditsdownstreamtargets,particularlyS6,invarioustumorcelllinesandxenografts.Hennessy,B.T.,etal."PharmacodynamicMarkersofperifosineefficacy."Clin.CancerRes.13:7421-7431(2007).
• Perifosineinducessignificantinvitroandinvivocytotoxicityinhumanmultiplemyeloma(MM),whichisassociatedwithdown-regulationofAktphosphorylationintumorcells.c-JunN-terminalkinase(JNK)playsacriticalroleinperifosine-inducedapoptosis.Perifosineenhancesdexamethasone,doxorubicin,melphalanandbortezomib-inducedMMcellcytotoxicity.Hideshima,T.,etal."Perifosine,anoralbioactivenovelalkylphospholipid,inhibitsAktandinducesinvitroandinvivocytotoxicityinhumanmultiplemyelomacells."Blood107:4053-4062(2006).
• NosignificantclinicalactivityofperifosineagainstandrogenindependentprostatecancerwasobservedinaphaseIIstudy.Posadas,E.M.,etal."AphaseIIstudyofperifosineinandrogenindependentprostatecancer."CancerBiol.Ther.4:1133-1137(2005).
• Twenty-threepatientswithadvancedsofttissuesarcomareceived66cyclesoftreatmentwithperifosine(1cycle=4weeks).The3and6monthprogression-freesurvivalwas22%and9%.Bailey,H.H.,etal."PhaseIIstudyofdailyoralperifosineinpatientswithadvancedsofttissuesarcoma."Cancer107:2462-2467(2006).
• Inchemicalstructureterms,perifosineisknownasa"betaine"or"zwitterion,"whichcanalsobereferredtoasan"internalsalt."Thesetermsareappliedtocompoundsthathaveanetneutralchargefortheentiremoleculebutwhichcontainbothapositively-chargedfunctionalgroup(suchasaquaternaryammoniumcationinthecaseofperifosine)andanegativelychargedfunctionalgroup,suchasaphosphateorcarboxylateanion.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,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.

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