LC Labs/R6399 Rucaparib, Phosphate Salt, >99%/R6399/50 mg

Rucaparib,alsoknownasAG014699,isapotentPARP1inhibitorwithaKiof1.4nM.ThomasH.D.,etal."Preclinicalselectionofanovelpoly(ADP-ribose)polymeraseinhibitorforclinicaltrial."Mol.CancerTher.6:945-956(2007).
Thisresearchcompoundisthephosphatesaltformofrucaparib.Wealsoplantooffertherucaparib,freebaseform;pleaseseeRucaparib,FreeBase,Cat.No.[R-6300].Thefreebaseformwillbeaddedtoourwebsiteassoonasthefirstlotisready.Thephosphatesaltformofrucaparibisusedforsomeorallrucaparibformulationsforuseinhumans.
RucaparibinhibitedthegrowthofhumancancercellsorxenografttumorswithmutatedorepigeneticallysilencedBRCA1/2.DrewY.,etal."Therapeuticpotentialofpoly(ADP-ribose)polymeraseinhibitorAG014699inhumancancerswithmutatedormethylatedBRCA1orBRCA2."J.Natl.CancerInst.103:334-346(2011).
Rucaparibenhancedthecytotoxiceffectsoftemozolomideandtopotecaninchildhoodneuroblastoma.DanielR.A.,etal."Inhibitionofpoly(ADP-ribose)polymerase-1enhancestemozolomideandtopotecanactivityagainstchildhoodneuroblastoma."Clin.CancerRes.15:1241-1249(2009).
RucaparibradiosensitizedprostatecancercellstolowdoserateradiationappliedoveralongerperiodoftimethatresultedinenhancedDNAdamage.ChatterjeeP.,etal."PARPinhibitionsensitizestolowdose-rateradiationTMPRSS2-ERGfusiongene-expressingandPTEN-deficientprostatecancercells."PLoSOne8:e60408(2013).
Antiproliferativeeffectsofrucaparibweredemonstratedin26of39(67%)ovariancancercelllinesandwerenotrestrictedtocelllineswithBRCA1/2mutations.Druginteractionswithrucaparibwereshowntobesynergisticfortopotecan,synergisticoradditiveforcarboplatin,doxorubicinorpaclitaxel,andadditiveforgemcitabine.IhnenM.,etal."TherapeuticPotentialofthePoly(ADP-ribose)PolymeraseInhibitorRucaparibfortheTreatmentofSporadicHumanOvarianCancer."Mol.CancerTher.12:1002-1015(2013).
Increasedvesselperfusionbyrucaparibmaycontributetochemopotentiationinvivo.AliM.,etal."VasoactivityofAG014699,aclinicallyactivesmallmoleculeinhibitorofpoly(ADP-ribose)polymerase:acontributoryfactortochemopotentiationinvivo?"Clin.CancerRes.15:6106-6112(2009).
Aphase1clinicaltrialdemonstratedthatthecombinationofrucaparibandtemozolomidewaswelltolerated.PARPinhibitionwasshownatalldoses.PlummerR.,etal."PhaseIstudyofthepoly(ADP-ribose)polymeraseinhibitor,AG014699,incombinationwithtemozolomideinpatientswithadvancedsolidtumors."Clin.CancerRes.14:7917-7923(2008).
Combinationtreatmentwithrucaparibandtemozolomideincreasedprogression-freesurvivaloverhistoricalcontrolsinpatientswithmetastaticmelanoma.PlummerR.,etal."AphaseIIstudyofthepotentPARPinhibitor,Rucaparib(PF-01367338,AG014699),withtemozolomideinpatientswithmetastaticmelanomademonstratingevidenceofchemopotentiation."CancerChemother.Pharmacol.71:1191-1199(2013).
Thisrucaparibproductisthephosphatesalt,whoseCASnumberisgivenabove.TheCASnumberoffreebaseformis283173-50-2.
AnotherCASnumberpreviouslyassignedtoRucaparib,PhosphateSalt,namely917828-48-9,hasbeendeletedbyCASandisnolongerinuse.
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.

M.W.421.36
C19H18FN3O•H3PO4
[459868-92-9]

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LC Labs/R6399 Rucaparib, Phosphate Salt, >99%/R6399/50 mg