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| @HAZLETON WASHINGTON AR226-0%5] GENOTOXICITY TEST ON T-5710.1 IN THE IN VIVO/IN VITRO UNSCHEDULED DNA SYNTHESIS AND CELL PROLIFERATION IN RAT LIVER CELLS [EINAL REPORT AUTHOR Maria A. Cifone, Ph. D. PERFORMING LABORATORY Hazl9e2t0o0n LWeaesshbiunrggtoPni,keInc. Vienna, Virginia 22182 LABORATORYPROJECT ID HWA Study No.: 15516-0-494 SUBHITIEDTO 3M Corporation Building 220-2E-02 3M Center ST. Paul, MN 55144-1000 SCTUODYMPLETIDOATNE September 14, 1993 15516-0-494 1 of 32 601293 2 WASHINGTON QUALITY ASSURANCE STATEMENT PROJECT TITLE: DGNeAnoStyonxtihceistiys Taensdt CoenllT-5P7r1o0l.i1feIrnatiVoinvo/iInnRaVtitrLoiveUrnscCheelldsuled PROJECT NO.: 20991 HHA STUDY NO.: 15516-0-494 PROTOCOL NO.: 494, Modified for 3H Corporation tQhuealiatbyoveAssruerfaenrceenceidnsppreocjteicotnsweorfethceondsutcutdeydanadccorredviinegw otof tthhee fSitnaanldarrdeport of gOepneerraatlingreqPuriorceemdeunrtess ooff tthhee QaupaplriotpyriaAtsesurGaonocdeLUanbiotratanodryaPcrcaocrtdiicneg troegutlhaetions. mFainnadginegmsentfraonmdthtoe tihnespsecttuidoynsdiraendctofrinaoln rtehpeorftollroewviinegw wdaetrees:reported to jonD Fini itor Perfusion/3-25-93 7D-ra6f,t7,r8e,p9o,r1t2-r9e3view/ F9i-n1a4l-9r3eport review/ 3-25-93 7-15-93 9-14-93 K. Newland B. Mullett B. Mullett 15516-0494 uaf%ityad AMssuurlanlce! Un atientReelseas 2 01294 WASHINGTON COMPLIANCE AND CERTIFICATION STATEMENT The described study was conducted in compliance with the Good Laboratory Practice Regulations as set forth in the Code of Federal Regulations (21 CFR 58, 40 CFR 792, and 40 CFR 160) and the Organization of Economic Cooperation and Development Principles of Good Laboratory Practice C(81)30 (Final) Annex 2, issued 1979-1980 (effective 1981). To the best of the signers' knowledge, there were no significant deviations from the aforementioned regulations or the signed protocol that would affect the integrity of the study or the interpretation of the test results. The raw data have been reviewed by the Study Director, who certifies that the evaluation of the test article as presented herein represents an appropriate conclusion within the context of the study design and evaluation criteria. All raw data, documentation, records, protocols, specimens and final reports generated as a result of this study will be archived by Hazleton for a period of at least one year following submission of the final report to the sponsor. After the one year period, the sponsor may elect to have these materials retained int the storage facilities of Hazleton for an additional period of time or sent to a storage facility designated by the sponsor. SUBMITTED BY: dee Z Hon Andrea L. Ham, B. S. Supervisor 9/4/53 Date Study Director: Prona 7 Lone: Maria A. Cifone,'Ph. D. Study Director 7 Division of Genetic and Cellular Toxicology 9-44-23 Study Completion Date 15516-0-494 6012395 WASHINGTON TABLE OF CONTENTS PAGE NUMBER ABSTRACT . LL . tee 6 L SPONSOR . . vt titties 7 I. MATERIAL TESTED . oo vv ttt tie eae ee eee uu 7 A. Genetics Assay No. B. Identification C. Physical Description D. Date Received TIL TYPEOF ASSAYS oo vvvit tein. 7 IV. PROTOCOL NUMBER . . . . . o.oo... 7 v. LL SE 7 AB.. SEtxupderyimIennittailatSitonartDatDeate Cc. Experimental Termination Date VI. AS.UPERVsItSuOdRyY DPiErReScOtNoNrEL . . . . . . uo www uuu uuu o 7 B. Scientist [HN Study Supervisor VIL OBJECTIVE oo ovt titties 7 VIIL DEFINITION . oo titi tiie tte e eee eee a 8 I MAA.TERIAILnSdic. at. or Ceiilsotitit iit... 8 CB.. MOsemdoitaicForPumUpDsS AasndsayLabel for Cell Proliferation Analysis D. Control Articles X. EXPERIMENT DESIGN (UDS ASSAY) . . . .. .............. 10 A. Dosing Procedure B. Dose Selection and Perfusion Time CDc.. UUDDSS AAnsaslayysis 15516-0-494 4 601296 g WASHINGTON TABLE OF CONTENTS (CONTINUED) XI. AE.XPERITMrEeNaTtmDeEnStIGNa:ndCEDLoLsePLReOvLeIlFsERATION ANALYSIS . . ........ 12 B. C. TIimspsluaentaCtoilolnectoifonOsmaondticPrePpuamprsation D. E. AsIsmemsunsomheinsttoocfheCmeilclal PSrtoaliinfienrgation Rates XII. ASSAY ACCEPTANCE AND EVALUATION CRITERIA: UDS . . . . ....... 13 XIII. ASSAY EVALUATION CRITERIA: CELL PROLIFERATION . . . ........ 15 XIV. INTERPRETATION OF UDS RESULTS . . . . ............... 15 XV. INTERPRETATION OF CELL PROLIFERATION RESULTS . .......... 17 XVI. CONCLUSIONS . . . o.oo tive iennnn.... 18 XVII REFERENCES . . . . ........................ 18 XIII. EXPERIDMATEATNATBLAESL. . . . . .. .............. 21 XIV. APPENDIX A: HISTORICAL CONTROLS . . . . . ............ 29 15516-0-494 5 C0129? @HAZLETON ABSTRACT The purpose of this study was to determine the hepatotoxicity and/or genotoxicity of the test material by measuring DNA repair as unscheduled DNA synthesis (UDS) and cell proliferation (CP) measured as S-phase induction in rat liver cells after in vivo treatment. The test material was administered mteoasruartsemeanttdoosfesbotohf UaDpSproanxdimacetlellypr81o0l,ife4r0a5t,io2n0.3, and 101 mg/kg for the The test material, T-5710.1 did not induce significant changes in UDS as measured by the nuclear labeling of rat hepatocytes. Primary hepatocyte cultures were prepared at two sacrifice times, approximately 2-3 hours and 15-16 hours after administration of a single oral dose. For each sacrifice time, three male rats were treated with test material suspended in corn oil. The hepatocyte cultures were incubated with 10 uCi/ml *HTdr for about 4 hours and autoradiography was performed the *HTdr-treated cultures. After autoradiography, three treatment groups from each sacrifice time were selected for analysis of nuclear labeling beginning with the highest dose where cellular morphology was adequate for analysis and proceeding to successively Tower doses. None of the criteria used to indicate UDS was approached by the treatments and no dose-related response was observed. The test material, T-5710.1 was therefore evaluated as inactive for the induction of UDS in rat hepatocytes after in vivo treatment and in vitro culture. In the cell proliferation assay, no evidence for an increase in cell proliferation was observed following treatment with the test material. Five animals per condition were labeled with BrdU for 72 hours using ALZET osmotic pumps. Samples of the liver and duodenum were fixed in 10% neutral Formalin and later embedded in paraffin. Samples were also processed for analysis by a pathologist. Sections from the left lateral, right median and anterior lobes of the livers as well as samples from the duodenum were taken and processed for immunohistochemistry. Each slide was prepared with sections from both liver and duodenum. The duodenum (a rapidly proliferating organ) was used as an internal control for delivery of label and immunohistochemical staining. The percentage of nuclei incorporating label in the liver was determined microscopically. Only hepatocyte nuclei were enumerated. No statistically significant increases in cell proliferation were observed. T-5710.1 was therefore considered negative for the induction of both UDS and cell proliferation in rat liver cells. 15516-0-494 6 0i238 2 WASHINGTON In Vivo/In Vitro GUennsocthoexdiuclietdy DTNeAstSyonnthTe-s5i7s10a.n1d iCnell Proliferation in Rat Liver Cells 1 SPONSOR: 3M Corporation 11. MATERIAL TESTED: A. Genetics Assay No.: 15516 B. Identification: T-5710.1 CD.. DPahtyesicRaelceiDveesdc:ripFteibornu:aryC2r4e,am19c9o3lored granular material III. TYPE OF ASSAYS: DNInAVSiyvnot/hIensiVsitrAossayRawtitPhriTmwaoryTHiempeaptooicnyttseanUdnscCehlelduled Proliferation IV. PROTOCOL NUMBER: 494, Modified for 3MCorporation v. STUDY DATES: A. Study Initiation Date: February 24, 1993 B. Experimental Start Date: March 4, 1993 C. Experimental Termination Date: May 6, 1993 VI. SUPERVISORY PERSONNEL: A. Study Director: Maria A. Cifone, Ph. D. BC.. SStcuidenytiSsutp:erviMsaorri:e MAcKnedorne,a LM.. HPahmi,l. B.S. VII. OBJECTIVE: The objective of this assay was to detect DNA damage and/or hepatotoxicity caused by the test material by measuring DNA repair as Seux-nipsshctahesenedcueliendadnudDcNtAidoengsryenienthoerfastiDsNlAi(vUeDdSra)macgeaelnldwseceraleflteirnpfrieornlrivefdievroaftriotomrneaant(mCePin)ntc.mreeaassTeuhreeidn as net nuclear grain counts in hepatocytes obtained from treated animals when compared to those from untreated animals. The types of DNA damage are ruenssupletcifiinedthebutinmcuosrtporbeatiroencogonfiznaebwlebasbeysth(einccelluldiunlgar*Hr-etphayimridsiynset)eminatnod DNA during a short (4 hours) in vitro culture period (1). Cel] proliferation measured the fraction of cells undergoing cell replication in rat liver using an immunohistochemical technique (2,3) to ATdnieivtmeearclstswbewrreoermeodigesioovxleayntuerdiadifsnoielnlgol(weBirnodgrUa)ladidmnoicsnoiersptoorfraatttiehoden tdoeufsrtiBnmrgadtUDeNrAfioarslyn72tahndehsoiutsrh.se in 15516-0-494 7 C01299 @ HAZLETON WASHINGTON yivo with an ALZET osmotic pump implanted subcutaneously. Quantification of cells that have incorporated DNA precursors over the 72-hour period measures cell proliferation in the liver (4). VIII. DEFINITION: The UDS assay is designed to measure unscheduled DNA synthesis (UDS) in rat liver cells (hepatocytes) using the autoradiographic technique described by Williams, 1980 (5). Hepatocytes were isolated from the livers of rats exposed in vivo to the test article. Only a small percentage of the cells enter S-phase (replicative DNA synthesis) during the brief exposure period, so the incorporation of *HTdr into DNA during n vitro culturing, as analyzed by autoradiography, may be used as a measure of the repair of DNA damage caused by treatment with the test wairtthiclken.own ThmiustagUeDnSicmeaosrurceamrecnitnogoefniDcNAarcetipvaiitrieasppeoafrschetmoiccaolrsr.elate well Hepatotoxicants such as carbon tetrachloride and dinitrotoluene induce an increase in cell proliferation to replace necrotic tissue (3,6). These proliferating cells may be detected during S-phase analysis. Other chemicals may induce S-phase in the absence of hepatotoxicity. It is not apparent how cell proliferation may act in thecarcinogenic process but there are numerous mechanisms which can be affected during replication (7-10). Chemically induced cell proliferation may increase the probability of spontaneous mutations as well as increase the probability of converting unrepaired DNA adducts into mutations. Unscheduled cell proliferation may also play a role in the expansion of preneoplastic populations leading to the emergence of a fully transformed clone of cells. Some of these examples act by a non- genotoxic mechanism and it is theoretically possible to detect nongenotoxic technique. carcinogens as well as genotoxic carcinogens using this IX. MATERIALS: A. Indicator Cells Young adult male rats of the Sprague-Dawley strain, 10-12 weeks old at the time of dosing, were purchased from Charles River Laboratories, Inc. (Cr1:CDBR). This healthy random bred strain was selected to maximize genetic heterogeneity and assure access to a common source. Animals scheduled for this study were housed according to standard operating procedures and were fed Purina Certified Rodent Chow (Formula 5002) Animals were quarantined a minimum of and water ad 7 days prior libitum. to random assignment to study groups and identification by tail tattoo. Animals were anesthetized prior to surgery for preparation of cell cultures, using about 60 mg/kg sodium pentobarbital, and were exsanguinated during the harvest procedure. 15516-0-494 8 C01300 ? WASHINGTON T3h2e4.5l-i4v3e9r.1ceglrlasmsforforthetheUDSeaarlsysaytiwmeeproeinotbtaaindned343f.r2o-m43r7a.t2s gwreaimgshing tfhoer Ttihveerlsatienr stiitmyepowiintth. a Tchoellacgelelnsasewerseoluotbitoanine(dseebySpecetrifounsioXn.C.of UcaDunSldtuAwrseesrsaey)wu.esreedMmotanhioenltasayaiemnreeddcauylastufrmoeorsnoalwnaeayrleeyrssiesstataobflabitoshuehtedUD3S7inCacctuiinlvtiuatrye. disAlhles humidified atmosphere containing approximately 5% CO. uFsoirngtheMetcoelflaneprol(imfeetrhaotxiyofnluraasnsea,y, Ptihtemana-nHiomoarles, weIrnec.)aneisnthhaeltaitzieodn wasenurebesctuhatneaesnsietaohuesatlniydzeo(dndeorwsiAatLlhZETCsOu,rfpaauncmdep)e.pxesraSneagvnueiimnnatalyt-etwdwaosprahiosouerrpsttioclaartleelmryo,vianalsneiormftaelds t1h0e% NTeiuvterrasl anBduffdeuroeddenuFmorm(acloinnt.rol organ). The organs were fixed in B. Media For UDS Assay mTheentecedllwitchult1u0r%esfetwaelreboevsitnaeblisserhuemd, i2n mWdillLi-agmlsu'tamMiendei,um10E0suugp/pmllewsittrheoputtomysceirnunsuilsfarteef,erraendd t1o50ausg/WmMiEI.genAtfatmiecrinthe(WeMEs+t)a.blisWhHmEesnt p47eriCoid/,mMoclueltu(rWeMsE-twreeraet)r.efed with WME containing 10 uCi/ml HTdr, C. Osmotic Pumps and Label for Cell Proliferation Analysis wAeLrZeETuseods.motiAcsipnugmlpes T(oAtLZA(0C4o22r0p5o)ratwiaosn,usePdalethArlosuog,houCtA),thMeodsetludy2.ML1 TThhee ppuummppshwaesrea p2r0e00-f1illecdapwaictihtyBrwdiUthata apumcponcreantteraotfio1n0 uo1f/hour. 20 ng/ml. D. Control Articles 1. Vehicle control Aandvehfiicvleeractosntrfoolr cceolnlsisptrionlgifeorfattihorneewerraetstrfeoartetdhebyUDSoraalssay 2g8a2v5a1g7e:5w9i)thwatshepveerhfiocrlmee,d catornalloiltim(e1p0oimnlt/sk.g, DVuekhei,cle control mhaenpiaptuolcayttieosnsorusteidssufeosr twheorseesduebrjievcetdedftroomaitlreaotfedtheanimals. D10osmiln/gkgv.olume of the vehicle control animals did not exceed 15516-0-494 9 01301 WASHINGTON 2. Positive control article TSFh-oeprhaptshoeesiUtiDniSvertaitcmoenhpteropoialnttoscc,yotmeDpsiomuienntdhvyiiIsvnoik.tnroowsTnahemtionpeoisnid(tDuWicNve,e UCDcASoSntorrol 62-75-9, Sigma Chemical Co., Lot# 29F0679) was dosed at 1105-m16g/khgourfsortitmheepo2i-n3t.hourFsortciemlelpoipnrtoliafnedra1t5iomng,/kg15 fomrg/ktgheof DainMndNtrwafapisevreiutsroeantdesaalsfortihncejeelcpltoisoipntriovfleoirfecoernaatctrhioolnt.imweeprToehirnteter.eartaetds bfyor UDS E. Test Article 10 mi/kg. For the preparation of the dosing solutions, the test article was suspended in corn oil at a concentration of 81.1 mg/ml and serial dilutions made prior to dosing for each timepoint and used fresh. The maximum dosing volumes for the test article did notexceed X. EXPERIMENT DESIGN (UDS ASSAY): A. Dosing Procedure For each tinepoint, three rats were treated by oral gavage with the test article. Delivery volumes were calculated on the basis of the most recent animal weight and the target dose. The maximum volume of the test article solutions administered did not exceed c1o0nmtlr/oklgs. werFeresuhsedprfeopraraatniyontsesotifngtespturpaorstei.cleCoinnfivremhaitciloen anodf the canodncdeonstirnagtioonf tohfetahessatyeswtasmatneortiadleteurnmdienredconinditcioonnjsuncotfipornepwairtahtion this study. B. Dose Selection and Perfusion Time bThaesedhigohnesLdt,,doisnefoorfma8t1i0onmgs/ukpgplwiaesd sbeyletchteedSpfoonrsorb.othTthirmeeepoints additional doses of test material were prepared using 2-fold dilution steps and a minimum of 3 animals per dose. Two taifmteeproitnhtes awdemrienisetmrpaltoiyoend oral gavage. offora sascirnigflieced;ose2-3ofhtohuersteasntd a15r-t1i6clehobuyrs c. 15516-0-494 UDS Assay This assay was based on the procedures in rats described by Williams (1980), Mirsalis, Tyson and Butterworth (1982) and pBeurtftuesriwoonrthofetlivale.rs (i1n98s7)i.ty Tfhoer habeopuattocfyotuersmwienurteesobwtiatihnedHabnyks' 10 C01302 2 WASHINGTON bbbuiasflfaen(rcse-daatmisnpaoHletts7h.y2(].CaeTMTthh-eenrM)g-W"NM-,EfIrNe-ceto)enttcraoainantciaenitgniic5n0g-a1c00i.0d5 u(mnEMiGtTesAt/)hm,lylaeonnfdegHlEyPcEoSl- omcifonlueltxaecgsie.sneadseThTei(vWehHrEeCp)taitsowscausyetepseinrwfeuarseecdulotbtuthrareionuedgdihshbtyhcemoenlctihavaiennriicnfagolrWHd1Ei0Cs.p-er1sT1ihoen csluusmppesndeadndtdiesbsruies.andThceellcsellwerseuspaelnlsoiwoend cell pellet resuspended in WME+. After wtaosscetetnlteriftuogerdemoanvde tcehlel obtaining a viable cell ccoounntta,iniangseraie2s5-momf r3o5u-nmdm, cpullatsutriecdicsohveesrsl(iapt animal to assess attachment efficiency) was alnedastat 6 lepaesrt an2impaelr inoculated for each paneirmadlishw.ith Ianpdpivriodxuiamlatecluyltu0r.e5s xwe1r0e tattoo: number. viidaebnlteifcieeldlswitinh 3thmel aonfimWalES Achneulmliadtictfuailcethdumreenasttmpofesorrpihoetrdheeoecfaorn1lt.ia8ei-rn2.i1ntgimhe5op%uorisCnOt,a.twaasbFoourustetdh3e7tolCaetistntearablish the tthiemepaotitnatc,hmeannt aptetraicohdm,entunaptetraicohdedofce1i.l7s-2w.0erehourresmowvaeds cultures were refed with 2.5 ml WHE-treat. Three of uasnedd.theAfter the replicate wrceeurpleltiucrkaeetspetsfrfoowremreaenauacshleydsainsitmoailnaswsteehesrseevauetsntetadchofmfoernttet.chheniAUcnDaySl arspesrmaoaybi;lneimntsgwowciuotlfhtutrhees acuulttourraedsiogfrraopmhye.achAtatniamcahlmenbty trypan blue dye exclusion to ienffsiictiuenmciycrwoasscodpeitcermainnaleydsifso,r two using determine the viability of the attached cultures. twAheferteerirnecafuebldaatboweriltihnfgoWrMpEe1Ir7i.o8cd-o1n8to.af9inaihbnooguurts0.42(52h-om3urMshotulhraysbmeildteiidnmeepcoeailnnldt)crueoltrtuurrn1ee8sd.3-to a1d8d.i8tihoonursof(11%5-1s6odihuomurscittriamteepoitnot)t.he Ncuocvleerisliwpesre(tchoenntaisnwionlglentheby tcehlrleemocnhoalnagyeesrso)f faocreti7c-10acmiidn:uettehsa.nol Th(e1:3c)ellasndwedrreiednexftorfaitxedleaisnt d2i4ppheodursi.n KoTdheakfNiTxBe2d cemouvlesrisolni,psanwderderimeodu.ntedTheonemgullasssionslicdoeast,ed dselviedelsopewdereinsDt1o9r,edfifxoerd,8 daanyds'sattain4edC.witThheheemmualtsoxiyolnisnwearnde etohseinn. D. UDS Analysis mtTahhegenivcfieidlcelaostiswocenrreeeunenxdaeomrfinaoienldaumitimocmmreaortssiiccoonpicocauanndltleytrh.eatfiUaeDpSlpdrwoawxsaismmaetdaeislsuyprlea1dy5e0db0xyon counting nuclear grains and subtracting the average number of 15516-0-494 1 C01303 WASHINGTON grains in three nuclear-sized areas adjacent to each nucleus (cytoplasmic count). This value is referred to as the net nuclear grain count. The coverslips were coded to prevent bias in grain counting. wTsuehnerelleeescnstseectodortnehcudeec,rlllwesiaasrnedongraianneiyadncihcoacctcoceauodsnv.iteornswalaOlisnplyndue(cnttluehecrrilemeeiinbecldwoaicvtkefheronsrelndiofrpimsfbaytlypegrmrraoairannpndshioommlaltoloy)ggies numerous to'count were excluded as cells in which replicative DNA synthesis occurred rather than repair synthesis. The average mean ntaehvteerantgrueicdplleiafcroartgereaacichnovectrroseulanittpmse(n+t(s15ct0oannddtioattriadolnd.neuvicalteiio)n)fowraseacdhetearnimmianled anfdrom XI. EXPERIMENT DESIGN: CELL PROLIFERATIONANALYSIS A. Treatment and Dose Levels AaaTnn1iamlayalznseiafclerslolnweeprarceohlidfdoeosrseaedtialosenvedleastcarn7id2b-ehcodounrtisrnolatfhetgerroUuDpSa wseercteiouns.ed tFoive single oral dose. B. Implantation of Osmotic Pumps A2aL0nZ0eE0sTt4h1etMioozdfeeldBrud2UsMiL1nagt oMasemtcootofinaccneenpturmaapstccioo(rnLdoiotnf#g2004to22m0gs5/t)maln.dwaerrdeThepprroeaclneoidamudareledsswweiartnehd o(ndeorspaulmp suprefracaen)i.mal Twhaes iancsiespitoincalwalsy cilnosseerdtedwistuhbcwuotuanndeoculsilpsy and ttihhmeeprleaanntiwemedarlestnhomreoencilitdnaoiyrcseadlpruinstoiigrlnstotohfesactirinimffeeicctoeif.ons.acrTihfeiceosmtootiecnsupruempsthwaetre C. Tissue Collection and Preparation Each aninal was anesthetized prior to removal of organs for aanndalyfsiixse.d duodenum, ainTthiensesuttuhreoarlwaictibhcuffhceiagrvheidtyceflwolarsmatluoirpnne.onveedrA,acnrwdoasstshealsselocitvierorenmroevomefodvefdrom ethaacth tahneimaTlabealndwafsixeadd.miniThseterdeudodeconrurmecwtalsy itnocleuadcehd aasnimaanl.indFiocratotrhe llaitveerr,al, urigphatrramfeidnianembaenddderdighstectainotnesriowrerelobteask.en Sfirmomilatrhley left prepared sections of the duodenum were also made and a section of the duodenum was mounted on each slide. Slides were also prepared atoccdoertdienrgminteo siftanadnayrdabnporromcaeldiutrieess fowrereexparmeisneantti.on by a pathologist 15516-0-494 12 01304 WASHINGTON D. Immunohistochemical Staining hematoxylin counterstain. Parallel slides were stained with The slides were deparrafinized and rehydrated prior tostaining using the BIOGENIX Supersensitive Kit using DAB stain and hematoxylin and eosin for analysis by a pathologist. E. Assessment of Cell Proliferation Rates Tthheat setchteioTnabeolf Tabel delivery wtahse was dcporunoofpdieerrnmlueymd,waadssmliinmdiiescstreorsfercdoompitotchaeltlheydifeafnxieamrmaeilnn.tedlOotnboecseenwseurree eToxbaemsinetdherfeofrorleobcuellalr dciofufnetrienngcewsa.s peLrafboerlmiendg wwiatsh ssiemcitliaornsanofnrgomthtehe left lateral lobe. The percentage of nuclei incorporating label in the Tiver was determined microscopically at approximately 400 gteone6r0a0tXedmagbnyifciocmaptuitoenr.. AThe1.a0rmemasstquoarbee cionudnetxeedd woceurlearragnrdiodmly divided into 10 x 10 squares was used to define the counting area. At Teast 2000 nuclei were examined per animal with a minimum of 3 sections and 8 fields per section. Any nuclei that were blue were considered unlabeled and any nuclei containing any brown chromogenic hue were considered labeled unless a clear artifact was present. Only hepatocyte nuclei were enumerated. Fields that contained areas of necrosis were not included in the evaluation. The slides were coded for (blind) evaluation as to treatmentgroup. S-phase nuclei labeling indices for each animal were calculated as follows: Labeled S-phase nuclei (LI)=nh o.oeflp abea ledtocynt ucle ei X 100 total no. of hepatocytes counted XII. ASSAY ACCEPTANCE AND EVALUATION CRITERIA: ups Astnahteiasstfseiaseytd.rneosrTumhlaitlsslyloiwnislltylinigbfemalaclyonnosofitdetrehenedcocmrapicatcseesrpitaaalbllleisttefesodtr beevlaolwuataireon of situations, so the study director must exercise scientific judgnent in modifying trheeliacbriiltietryiaanodr cacocnespitdaenrcien.g other causes that might affect assay 1. 15516-0-494 The viability of the hepatocytes collected from theperfusion process normally exceeds 70%. A variety of factors can affect cell yield and viability, so values below 70% are not uncommon nor necessarily detrimental. Toxicity of treatment with test article may be reflected inperfusion viability, therefore no lower limit will be set. 13 C01305 ? WASHINGTON 15516-0-494 2. Tahsesayvitarbeialtimteyntosf mtuhsetmboenol7a0%yerorceglrleatceurl.tureNsormuasleldy,fotrhethe viability of attached cells is about 85%. 3. Tphoepulpaotsiiotniveemcpolnotyreodlwaiss ruseesdpontsoivdeemoanndstrtahteemetthhaotdotlheogycelwlas caaduesqiunagtewefaokr torhendoetUeDcStiaoctnivoiftyU,DS.theFoarvertaegset mreastpeornisaelsto the tpoosiitnidviecatceontUrDoSl. trFeoartmteensttsmmatuesrtiaelxsceecdleabroltyh ccaruistienrgiaaudsoesdearbesleantceed oUfDSaacptoisviittiyv,e canontarsoslaylwoisltl fobre ateccchenpitcaabllereiansotnhse. 4. oGfraitnheceouvnatluadtaitoanobitfaoibnteadinpeedr fanriommaltwoisreapclciecpattaebleculasturpeasrt baendaavtaillaebalset 5f0ronnuc2leoif ptheer c3ulatnuirmea.ls Gtrreaaitnedc.ount data should 5. Atimmeipnoiimnutm. ofR3epedaotsetrTieavleslsnewieldl onbleyaanuaglmyeznetd tahteenacuhmber of oafna3lyzdeodsedloesveellseveblust miunsttheincfliurdset attrialleastto oancehideovseea total previously assayed as acceptable. Sbeavseirsalforcrietvearliuaatihoanveofbeeanteessttambaltiesrhieadl whasicha,ctiivfemeitn, thperoUvDiSde a asstsaatyi.sticTahle canrailtyesriisa foofrthaephoissittoirviecarlesdpaotnaseanadrecbaalsceudlatoinona of the dmeisncirmiubmedinbcyreCaasesciraenqouiraendd fGoayrlaorsi(g11n)i.ficant UDS response as tThhaettceasutsem:aterial is considered active in the UDS assay at doses 1. fAniveingcrraeiansse pienrtnhuecmleeuasn anbeotvenuctlheearcognrcauirnrenctounntegattoivaet least control average, leading to a positive number and/or 2. Tihnecrepaesrecenatt olfeasntucl1e0i% waibtohveftihvee aorvermaogree oneftthgeraicnosncutrorent negative control animals. Galesnoerablelym,et.if Htohweevfeirr,stscaotnisdfiatcitoinonisofsatoinslfyieodn,e ctohnedisteicoonndcawnillalso vianrdiiectayteofUDSnucalcetiavritlya.beliDnigffepraettnetrnDsN,A-daandmagwienagk aaggeennttss can may give a strongly caofnfdecittioonnslyaraemcionnosriidteyreodf tihneancelelvsa.'luatTihoenr.eforIen,cabsoetsh owhfertehe above wiinlclreabesesconasreidenroetdobascetrivveedfoirn talhlatthcornedeitainoinmalisf, cetlhlestefsrtommattweorioafl 1 G01306 @ HAZLETON WASHINGTON the three animals show increases. show an average Tess than -5.00 or If the negative control animals more than 1.00 grains per nucleus, the assay will normally be considered invalid. The the test material is above conditions considered are met in inactive in this assay if none any of the treated animals. of When results the presence are neither clearly of a dose response, positive nor clearly negative, the frequency distribution of cellular responses, and is considered; the test the reproducibility of data article is then classified among slides "weak positive" or "equivocalTM. as "negative", A group in which one ofthree animals case by shows increases in nuclear Tabeling will be decided on case basis depending on the level of activity in cells a from the active animal, the level of activity in cells from the inactive animals and the presence or absence of activity in surrounding groups. The positive control nuclear labeling: is not used as areference point to estimate mutagenic or carcinogenic the UDS activity of the test material. UDS risk associatedwith elicited by test agents in this assay is probably more dependent on the type of DNA damage inflicted and the available repair mechanisms than on the potency of the test agent as a mutagen or carcinogen. Some forms of DNA damage are repaired without the incorporation of new nucleic acids. Thus, the positive controls are used to demon- strate that methodology the was cell population employed was responsive adequate for the detection of UDS. and the XITI. ASSAY EVALUATION CRITERIA: CELLPROLIFERATION XIV. A mean and standard deviation for the percentage terminal body weights and terminal liver weights of S-phase cells, were calculated for each treatment Jou Statistical analysis using the individual animal was performed using one-way mean values. analysis of variance techniques (12). Control versus treatment group comparisons were done with rank Dunnet's t-test transformations (13, 14). In the case of variance heterogeneity, of the data were performed prior to analysis of variance and Dunnet's t-test. An S-phase, terminal body weight or terminal liver weight percentage in a dose group that deviates from the percentage in the concurrent control group at a significance level of Pps0.05 was considered significantly different than the control group. INTERPRETATION OF UDS RESULTS: At the request of the Sponsor, the test material, T-5710.1 was suspended ainppecaorrendoitlo aftorma acocnrceeanmtractoiloonredo,f 8o1p.a1quemg/vmils.cousThesutsepsetnsimoanteriinalthe vehicle. Individual dosing stocks of 81.1, 40.6, 20.3 and 10.1 mg/ml 15516-0-494 15 01307 @ HAZLETON WASHINGTON were prepared just prior to dosing. Three rats per dose level were treated with 810, 405, 203, 16 hours groups, in volumes and 101 mg/kg which did not for both the 2-3 exceed 10 ml/kg. hours and 15- For the early timepoint, perfusions were initiated 2.1-2.6 administration of a single dose of the test material. The hours after hepatocytes bcloulelecetxecdlusfioorn)thefrUoDmS7a8s.s2a%y-98r.a6n%gedof itnhevitaobtiallitycel(ldsetceorlmliencetdedby intrythpean perfusate (Table 1). and the viability of The attachment efficiency varied the attached cells was very good, from 61.5%-104.1% ranging from 88.9%-97.5%. The minimum criteria for a UDS response at this timepoint were determined by comparison to the averages of the control treatments (Table 2). The average mean concurrent negative net nuclear grain count for the vehicle control animals was -0.32 cells containing five or more net nuclear and the average percent of grains was 3.89%. Apositive response consisted 4.68 (5 net grains of average mean net nuclear above the control value) or grain counts exceeding at Teast 13.89% of the nuclei containing five or more grains (10% above control value). "None of the treatments with the the average negative test material samples caused nuclear labeling control. Furthermore, significantly no dose-related different trend was from thenegative evident. Incontrast, the DMN treatments induced large increases in nuclear labeling that greatly exceeded both criteria used to indicate UDS. Since the positive control animals were responsive, the test results were considered to provide conclusive evidence for the lack of UDS induction by the test material samples at the 2-3 hours timepoint. Heavily-labeled nuclei (blackened with numerous undergoing DNA replication (S-phase) as opposed grains) represent cells to DNA repair. For each slide phase canaallcyuzleadt,ed atandlearsetpor5t0e0d ceflolrs ewaechreansicmaanlnedon antdhe tbhaesiisncoifdenatce loefastS- s1t5u0d0y cwealsls loowbsearndveddid(Tnaobtlein2)t.erfeTrhee wniutmhbertheparsesseanyt. in the 2-3 hours aFodrmintihsetrlaattieorntoimfepaoisnitn,glepedrofsuesioonfs twheeretesitnimtaitaetreidal1.5.2T-h1e5.h6ephaotuorcsytaefster collected for the UDS assay ranged in viability (determined by trypan blue exclusion) from perfusate (Table 3). 79.5%-92.2% of the total cells collected in the The attachment efficiency varied from 60.9%-91.1% 8a3n.d5%t-h9e7.v9i%a.bility of the attached cells was very good, ranging from cThaelcumliantiemdumbacsreidteruipaon ftohre aavUDeSragreesopofnsteheatnegtahteivleatceornttriomlepaoniinmtalwsas for the 15-16 hours timepoint -0.54, average percent of (Table 4; average mean net nuclear grains cells containing five or more net nuclear = grains = 2.50%). exceeding 4.43 or The criteria were at least 12.5% of mean net nuclear grain counts the nuclei containing five or more 15516-0-494 16 .01308 @ HAZLETON WASHINGTON grains. nuclear None of labeling the treatments with the significantly different test from material samples caused the negative control and no dose-related trend was evident. induced large increases in nuclear The positive control treatments Tabeling exceeding both criteria used to indicate UDS. Since results were considered the positive control animals responded, the to provide conclusive evidence for the lack test of UDS induction by the test material samples at the 15-16 hours timepoint. Huenadveirlgyo-ilnagbeDlNeAd rneupcllieciati(obnlacaskenoepdpowseidthtonuDmeNrAoursepagirra.ins)Therenpurmebseenrt cells observed for each animal in the interfere with the detection of 15-16 UDS. hours study was Tow and did not XV. INTERPRETATION OF CELL PROLIFERATION RESULTS: A. General Observations Cells stained with the brown DAB chromogen were observed in the dunusocdheenduumlefdromdeaatllhs ofocctuhrereadn.imalTshe usperdeseinncethoefstluadbye.l No in all the animals indicated proper delivery of the BrdU label andacceptable immunohistochemical staining. control) was eliminated from One animal from Group the evaluation because 1 of (vehicle extremely high time labeling than the indices. This animal other animals and may was treated at adifferent have been dosed improperly. One animal from Group 6 (positive control) was also eliminated from the study because the results demonstrated a lack ofresponse by the animal. Since DMN is known to induce large cell proliferation (15), this may have represented increases in a dosing error. The liver different weights of the dosed from control animals animals were not significantly and no obvious changes were observed at autopsy. The mean liver weight of the positive control was slightly elevated (p < 0.05) the large increase in DNA synthesis (and as. expected considering subsequent cell proliferation) that was occurring. 5) had a mean terminal body weight The that high dose animals (Group was less thancontrol value (p < 0.05) indicating some toxicity. Slides from treated and control animals gross findings at the time of sacrifice were were also examined and generally sporadic and/or incidental with no apparent relationship to treatment. 15516-0494 17 0L1309 ? WASHINGTON B. Summary of Labeled Cell Counts for the Liver ATlaabbsleuelmimna5.gryionIfdnedxitvhie(dLuIla)albfeolarneidmeaaclcelhlcgoruconoutupsntsiasrefporsrehsoeewannctheidgnroiTnuapbtlheies6.tshhiorTwdnhe imnean ncTeooclbruemosns.iasndwTathsheereoblswaeabreslvendwo.asapTprhaaernednontmecrwpoirtteihfcienreantrtheieaasllwoebleraseb,elnieonxtgceedpitbnutwahneynroetof the included in the count. Tsihynendtihmceeasatienss bdtauhcraktignrgoTuentsdhsetlh7aab2ne-lhio1nu%grofilnatbdehelxeinn(guGcrlpoeeuirpioh1d)a.d wausNnode0r.s6gi1ognneiwfhiiDccNahAnt ainndcrealalsesmeawnerelaobeblsienrgvedindiincetshewedroesedbelgorwoup1s% w(hGircohupsis2etxhpreocutgehd 5f)or c1o2n-twreoelk oanlidmamlaslewarsats3.1.51Thewhmicehanislabseilginnigficianndtelxyofeletvhaetepdositive (p 50.01). dTiohnsecesreeaastreesscuolnitncsenttdhreeamtoLiInosntisrnattfehreomthla1it0v1eTrm-g5i7/n1k0gm.a1lteod8ri1ad0tsnmogta/fktigen.rducaeLasrsigniegglneifiorcaalnt cionnctrreoalsesaniimnaltsh.e lTahbeelimneganinldaebxeliwnegreionbdsexervoefdthien tphoesitpiovseiticovnetrol animals was 31.51. XVI. CONCLUSIONS Tnhuecletaerstlmaabteelriinagl,ofTr-a5t710p.r1imadriyd hnoetpationcdyutceessaitgniefiitchaenrtthcehan2g-3eshoiunrsthe mtgi/mkegpowienrteodreltihever1e5d-16byhooruarls as inactive in the induction gtaivmaegpeo.int of UDS in ~wTh-e5n71d0o.1seswasoft8h1e0r,efo4r0e5 rat liver cells. eanvdalu2a0t3ed TSh-ephatseestcmealtlesrifaollldoiwdingnota were Tabeled for 72 hours siinndgulcee osriaglnidfoisceantofchT-a5n7g1e0s.1i.n following dosing and all mean tThheenaunmibmearlsof labeling indices opifonsaicttthiievveetrcienoanttetrdhoelgrioanundpiusmcatwlisoenrewaosfbe3Dl1No.Aw51s.1"%y.nthTe-Ts5hi7es10m.ei1annwraalstabetTlihivenergrefociernledlesxe.vaolfuattheed as 15516-0-494 18 01310 ? WASHINGTON XVII. REFERENCES 1. rgMieerpnsaoaitlroixsia,cssacJya..rcc.i,nEonTgvyeisnroson'n,.inCM.uKt.th,aegeiannnedsviiBsv.,Eo.4-:B5iu5nt3t-ve5ri6wt2or,roth1h:9e8p2a.tDoectyetcetioDnNAof 2. Defazio, (1987). vivo. J. AI.m,unLoehairsyt,ocJh.eAn.i,caHledldeeyt,ectDi.oW.n oafndprToaltitfeersraaltli,ngM.cHe.iNl.s Histochem. Cytochem. 35, 571-577. in 3. p5Lra-onbilreiorfn,eordaeTt.oiLx.oy,nurisBdteiurdgnieeers,a.ndET.oK-.xt,ihcyoamlniodgdiEisantceho9f,,n 6Pr4..oId.en(t19h8e9p)a.toCcoemlplaurliasron of 4. fMBoiurrtstaetlrhiweso,ritnhJ,.v,ivBo.PEr.or,basttA,shhebp6y.a,,tocJay.n,tde B6.DeNrAmW-uidlrelezip,aamisrE:.,assACaaysp.crioatnoMocu,otlatDi.a,onnd guide Res. 189:123-133, 1987. S. MDuWNitAlalgireaenmpssa,,iVrGo.alMn..d:6m.utTahgeF.endeDesetiescSteriironenslioavfnedrchcAe.umlitcHuaorllelsam,untdaIengr:e,nsC-(hcEeadsmr.ic)ci,anlogPelnesnunby Press, NY, pp. 61-79, 1980. 6. dDMiiNnrAistaslryionstt,ohleusJe.inCse..inanCdraartBcuihtnteoepgraewtnooercstyihts,e,sB3.f:Eo2.l:4l1o-w2iI4nn5gd,uicnt1i98ov2ni.vooftruenastcmheendtulewdith 7. DRMNaeArlsamtsaiynon,nthsehDsi.iSps.,otfoCahtettphlaeetyih,cepapR.teCor.co,axirscCooinmnweoagyep,nrioclJii.Gtf.ye,raotfainodtnhePoapnppde,rorxJei.pAsl.oimcea(t1i3v8e8). CXpayrn1ociledirifneoRr)eas-t.2o-rps4y8,rdiim6(i72d3-i9en-ty6hl7y4tl4hh.ieox]yl)apcehttihcalaactied an(dWy-[144-,c6h4l3o)ro-in6-(r2at,s3.- 8. WcCaarrnawcdiedcrok,c,k,IGn:.VP..M",.liEv(le1sr9e7v6Ci)ee.lrl, CCeaNlnolcretrhp"r,foiloiClaflmeaernrdaotniB,oionmHe.adMni.dc,aelLxipnPesrreeilsmlse,,ntaCl.A.liavnedr Ansterdan. 9. CRoelquumibraenmoe,ntA.o,f carcinogenesis cRealjlalapkrsomlii,ferS.a,tioanndfSoarrmtah,e Di.nSi.tRi.ati(o1n981o)f. as assayed by three different procedures. liver Cancer Res. 41, 2079-2083. 10. doGilfaimnloiisnv,oebreAn.rzDee.gn,een.eBruJat.cthieoErxn,p.onNM.eLtd.u.moR9r.,33f,oarn3md1a3tA-iu3bo2,n4.Ji.nC.rat(s195f1e)d. 4-The effect 15516-0-494 19 C0131 2 WASHINGTON 11. DCeNavAsacliuraaentpoia,nigrD.acAsh.seanyia.cnadlsMDu.Wta.astiGpooansyiltoRiersvee(a1ro9cr8h3,)n.e1g2a2tSitv8a1et-i8si5tn.ictahle cherpiatteorciyatefsor 12. DMeisniearn,, BM.Jc.Gra(w1-9H7i1l)l.,StNeawtiYsotrik,calznPdriEndciitpiloens,ipnp.Exp14e9r-i2m2e0ntal 13. Dcuonmnpeatrti,ng C.sWe.ver(a1l955t)r.eatmAenmtusltiwiptlhe 50, 1086-1121. caocmopnatrrioslo.n Jp.roAcme.durSteatf.orAssoc. 14. Dcuonnntertotl,. CB.iWo.met(r1i9c6s4).20, Ne48w2-t4a9b1l.es for multiple comparisons with a 15. Hsaantmdu,dyMoA.lleicvauenldrarCeifMffuoetnceat,gsenMie.nsAd.iusce(d1179(9b11y)9.)a, siU1n6s.geleofdocselel opfroDlMNi.ferEantviiornonmteontal 15516-0-494 20 01312 @ HAZLETON WASHINGTON XIII. EXPERIMENTAL DATA TABLES 15516-0-494 ' 21 01312 WASHINGTON TABLE 1 SUMMARY OF CULTURE DATA FROM IN VIVO/IN VITRO RAT HEPATOCYTE UDS ASSAY 2-4 HOUR TIMEPOINT Client: 3M Corporation Client Code: T-5710.1 -_-- HUA Assay No.: 15516-0-494 Trial Initiation Date: 23-Mar-93 TCeosntdition ANnuimmbaelr DToasregetLevel(1) --- VPiearbfiulsiitoyn AEtftfaiccihemnecnyt(2)AtVtiaabcihlmietnyt(2) Vehicle Control - Corn 011 (ml/kg) 34449 10.0 34448 10.0 34447 10.0 Positive Cont3r4o4l43 1 - D1MN0.(m0g/kg) 34442 34441 10.0 10.0 Test Material - (mg/kg) 334444337 881100 34435. 810 34425 34424 34423 405 405 405 34413 34412 34411 203 203 203 3401 101 34400 101 -_-- 34399 101 78.2 82.8 86.1 87.6 77.2 93.3 8835..32 8.3 79.4 87.2 90.9 91.3 85.7 98.6 98.0 83.5 87.9 92.3 83.9 67.6 72.5 76.5 78.1 8849..67 743 75.1 75.9 79.6 86.0 62.8 63.3 70.2 61.5 104.1 93.5 94.5 90.4 92.3 92.6 93.0 9952..29 92.8 92.0 88.9 93.1 95.2 95.5 95.3 97.5 2.3 94.6 N(o1)tesT:hree animals per dose level were treated. (2) Results based on viable counts (trypan blue dye exclusion) of randomly selected areas on two plates. DMN = DimethylInitrosamine 15516-0-494 : 22 C013ia @ HAZLETON WASHINGTON TABLE 2 SUMMARY OF UDS DATA FROM IN VIVO/IN VITRO RAT HEPATOCYTE UDSASSAY 2-4 HOUR TIMEPOINT CT lCtentCCToe:-- T510t .1 saaTetau) inis tiatioi nDatee : o3ts arss Client: 3M Corporation Client Code: T-5710.1 HWA Assay No.: 15516-0-494 Trial Initiation Date: 23-Mar-93 C --_ W mew Test Animal Cond. Number Target Dose * Mean Net Nuclear % Cells Grains He) w/ 25 + SI NNG Mean Percent Cyto. ~~ S-Phase Grains* Cells Vehicle Control 34449 34448 34447 - Corn 0i1 10.0 10.0 10.0 (ml/kg) -1.17 + 0.48 0.47 + 0.51 -0.27 + 0.24 2.00 6.67 3.00 6.00 4.61 4.63 0.20 0.47 0.30 Positive Control 1 - DMN (mg/kg) 34443 10.0 16.10 + 0.76 34442 10.0 15.66 + 4.30 34441 10.0 13.13 1.77 96.00 95.33 92.67 8.95 6.41 Nn 0.07 0.87 0.13 Test Material 34437 34436 34435 34425 34424" 34423 34413 34412* 34411 (mg/kg) 810 810 810 405 405 405 203 203 203 0.17 + 0.41 -0.03 + 0.70 0.24 + 0.00 -0.07 + 0.64 -0.51 + 1.37 -0.89 + 0.81 -0.23 + 2.11 0.62 + 0.03 -0.52 + 0.87 2.00 6.67 4.00 4.00 4.00 2.00 7.00 9.00 6.67 4.86 5.68 4.89 4.39 4.04 6.58 1.72 5.07 7.15 0.13 0.13 0.20 0.40 0.50 0.30 0.50 0.10 0.13 oT a TR --F-- uERiRmEiSL EtTEeTeohsnaeS Slt SrneLinStGy-- SSyceeIootE2c0cCoStrctTotiLsAcaIt(Tt1)6)wvroTtrcytAmr,sSiacinote {Nerv of Sygate grain coms an triplicate covrstpe C150 tat etl. 15516-0-494 23 01315 @ HWAASZHLIENGTTOONN TABLE 3 SUMMARY OF CULTURE DATA FROM IN VIVO/IN VITRO RAT HEPATOCYTE UDS ASSAY 15-16 HOUR TIMEPOINT Client: 3M Corporation Client Code:T9701 Client Code: T-5710.1 HWA Assay No.: 15516-0-494 TrTiriaall InIniittiiaattiioonneDaatetee:: o255-mMaarr--9s3s JT Test Condition Animal Number eeeh Target Dose Level(1) MeyErrielns@ aie Perfusion Attachment Attachment Viability Efficiency(2)Viability(2) Vehicle Control 34452 34451 34450 CORN OIL (ML/KG) 10.0 10.0 10.0 81.6 86.9 88.1 75.1 89.7 66.3 83.5 97.9 92.0 Positive Control 1 - DMN (MG/KG) 34446 15.0 34445 34444 15.0 15.0 80.3 86.2 89.6 79.4 60.5 68.2 88.4 92.5 93.1 Test Material - (MG/KG) mm gE es 34440 34439 34438 34428 34427 34426 34416 34415 34414 34404 34403 34402 810 810 810 405 405 405 203 203 203 101 101 101 87.4 82.9 80.2 79.7 88.1 92.2 79.5 89.7 85.1 92.1 85.9 87.3 91.1 76.6 66.9 76.6 72.4 79.5 73.5 82.6 60.9 75.0 83.3 85.5 93.9 94.4 86.8 93.7 91.0 97.1 89.7 95.6 89.1 93.9 96.5 95.7 Notes: (1) Three animals per dose level were treated. (2) Results based on viable counts (trypan blue dye exclusion) of randomly selected areas on two plates. DMN = Dimethylnitrosamine 15516-0-494 24 01316 WASHINGTON TABLE 4 SUMMARY OF UDS DATA FROM IN VIVO/IN VITRO RAT HEPATOCYTE UDS ASSAY 15-16 HOUR TIMEPOINT Client: 3M Corporation HWA Assay No.: 15516-0-494 Client Code: T-5710.1 - _-- Test Cond. Animal Number Target Dose * Trial Initiation Date: 25-Mar-93 nnn Mean Net Nuclear % Cells Mean Percent Grains (MNNG) Ww 25 Cyto. ~~ S-Phase + SD NNG Grains* Cells Vehicle Control - CORN OIL (ML/KG) 34452% 10.0 0.04 + 0.37 34451 10.0 -0.73 + 0.68 34450 10.0 -0.73 + 0.40 4.00 2.67 1.33 3.61 6.69 4.55 0.00 0.27 0.00 Positive Control 1 - DMN (MG/KG) 34446 15.0 3.95 + 2.86 34445 15.0 4.05 + 3.38 34444 15.0 5.01 + 2.62 38.67 38.00 48.00 2.59 4.58 3.32 0.00 0.07 0.07 Test Material 34440 34439 34438 34428 34427 34426 34416 34415 34414 (MG/KG) 810 810 810 405 405 405 203 203 203 -0.29 + 1.40 ~0.40 + 0.48 -0.24 + 1.07 -0.10 + 0.23 0.75 0.20 -0.40 + 0.12 0.43 0.40 0.63 + 0.41 0.05 + 0.54 9.33 1.33 6.67 3.33 7.33 2.67 7.33 7.33 7.33 8.54 5.26 5.79 5.47 4.54 6.67 5.21 5.46 1.37 0.07 0.00 0.00 0.00 0.27 0.13 0.27 0.13 0.07 (A-- Fr0eietateanoinFmaCtnoeeverpmaatiio-- er,ne rLeaNvetethlLSsaoaretrcr3uac-- reasar,pOicBaecoRvrietoi-- eraC1s50coaranl pcliee)-- ityh saunrda ddeveiattioen r ratcies oF cll (Gresko hor con te 3 ot mie arn n Bete vst 2 oimeBeciECo0rda R0yofitSSnoElttaEanrSalatoyciclnsesegwrooarisnrscaasmtemsrioanootnfeispeptwiencraWteeGncncoeveeorsfiiopaen w2(c15o0vSeotrttaeildpacaCt1t0y0. served shen total celles. 500 cls par 15516-0-494 25 001317 WASHINGTON Client: 3M Corporation Client Code: T-5710.1 Table Cell Proliferation Sumary HWA Assay No.: 15516-0-494 Trial Initiation Date: 5-Mar-93 Group/Sex | Dose Level | Labeling Indexb (mg/kg) (%) Liver Weight | Terminal Body (9) Weight (g) me od 0.61% 0.18 16.42 1.21 | 421.6 13.6 TM 101 0.49 0.46 17.16 + 1.46 420.0 + 23.7 3M 203 0.26 + 0.26 17.24 + 1.17 407.5 + 20.6 Mm 405 0.50 + 0.38 18.48 + 3.06 389.1 + 40.8 SM 810 0.34 0.25 18.32 1.10 365.1 + 24.6% 6HC 158 | 31.51% 15.86%| 19.48 + 2.06%| 459.8 + 30.1 "`PFievrecenatnaigmealsofpelrabeglreodupheupnaletsoscytiendniuccalteeid per total number of hepatocytes counted "(Faotur aTneiamsatls20p0e0r) group ""VPeohsiictlievecocnotnrtorlo,l, 1015mlm/ak/gkg ofofcDorNn oil *Significant atp < 0.05 *+ *SIingcnrieafsiecanitn tahte pm<ean0.01 4 Decrease in the mean 15516-0-494 2% 01318 WASHINGTON AnHuimmbaelr 33459 3344446610 34463 GGrroouupp MSeDan N 3344446645 34466 34467 34468 GGrroouupp MSeDan N 34469 3344447701 34472 34473 GGrroouupp MSeDan N Gr[Soeuxp m TMIMMH M2M 2M 2M 2M 3M E3dH 3MMn Cell ProlTiafbelreat6ion Assay Individual Animal Data MLeabaenl ing ndex_(%) 0.62 00..8612 0.38 0.0.6118 4 01.2149 0.62 0.19 0.19 00..4496 5 0.43 00..0150 00..1607 00..2217 5 TBeordymiWneailght (a 432.0 442092..92 422.2 4211.36% 4 443209..79 425.2 435.8 378.2 42203..07 5 303.0 34921..10 440082..59 40270.056 5 LiTveerrmiWneailght (a) 16.02 1147..8294 17.53 161..4212 4 1167..3646 17.85 18.85 15.10 171..4166 5 16.21 1188..5116 1175..4856 17.24 117 5 15516-0-494 27 01338 WASHINGTON Animal Group Mumber ___jsex 34474 aH 34475 an 34476 aM 34477 aM 34478 aM NGGrroouupp SMDean 34479 SM 34480 5M 34481 5M 34482 5M 34483 5M Group Mean GNroup SD 34514 oH 34515 6M 3344551176 66MM Group Mean Group SD N CelTlabPlreol6if(eCroanttiionnueAds)say Individual Animal Data LaMbeaenling Index () 0.95 0.19 0.29 0.19 0.86 00..5308 5 0.29 0.24 0.29 0.76 0.10 0.34 05.25 22.14 47.43 1442..2244 31.51 15.86 4 BToedryniWneailght (a) 401.6 369.9 379.8 342.6 451.4 3809..18 5 346.3 375.2 369.1 398.6 336.2 365.1 245.6 499.3 448.5 442683..03 459.8 30.1 4 LiTveerrniWneailght qq 20.22 14.87 18.83 16.06 22.42 183..4086 5 17.80 19.22 17.57 19.75 17.26 18.32 51.10 22.09 19.45 1197..3016 19.48 2.06 4 15516-0-494 2 C01320 @ HAZLETON WASHINGTON XIV. APPENDIX A: HISTORICAL CONTROLS 15516-0494 29 C0132 ? WASHINGTON HISTORICAL NEGATIVE CONTROLS IN VIVO/IN VITRO UNSCHEDULED DNA SYNTHESIS ASSAY Number of data points is 20 Animal # --_-- UDS Grains/ Nucleus + SD *% of Nuclei with 25Net Nuclear GrainsA*v*eGrraagiensCy*t*o FW Tein Erm 1 2 -0.23 -1.39 0.33 30.49 2.7 0.0 6.17 7.76 3 4 -0.99 0.47 0.12 30.89 1.3 4.7 8.19 7.69 5 6 -1.43 0.55 10.76 10.45 0.7 0.0 10.61 3.55 7 8 0.67 0.32 0.11 20.63 0.0 0.0 3.93 2.66 9 10 -0.11 20.25 -0.05 0.39 0.7 0.0 2.66 4.25 1 12 -1.05 -0.01 0.31 0.89 0.0 6.7 2.79 7.55 13 1 -0.38 -0.27 0.30 20.22 1.3 2.7 8.55 6.58 15 16 -1.38 -0.18 0.31 0.33 0.7 4.0 9.89 8.18 17 18 -0.57 0.34 -0.21 0.47 33 2.0 8.97 7.94 19 20 -0.59 0.38 -0.62 0.52 --_---------- 0.0 0.0 7.75 7.20 en Average: -0.52 spa 40.50 1.5 11.0 6.56 $2.44 Range: Low High -1.74 0.12 0.0 6.7 2.66 10.61 -_-- * gDaSte = oArvedruapgleicaotfe nceotvenrusclliepasr g(r1a5i0nceclolusn)ts a+nalsytzaenddarfdor daevisaitnigolne from triplianimal. ** a ASDver=agSetanvdaalrudesDefvoirattiroinplicate or duplicate coverslips for a single animal. 15516-0-494 30 COLuRL 2 WASHINGTON HISTORICAL POSITIVE CONTROLS IN YIVO/IN VITRO UNSCHEDULED DNA SYNTHESIS ASSAY 4-Hour Timepoint Number of data points is 9 AT -n_i--mal # NUuDcSleGursai5nsD/ * m %NetofNNuucclleeair Gwriatihns25** GArrvaeirenasgme**Cyto 1 2 22.27 23.25 42.36 1.08 98.0 98.7 7.46 7.01 3 4 22.25 19.44 11.96 20.75 10905..03 5.84 8.43 5 6 24.03 14.22 29.75 47.98 98.7 96.0 4.99 5.26 7 8 19.05 17.47 1.76 1.78 98.0 98.0 6.56 6.65 _F --9 16.83 S 4.00 R 97.3 5.74 Avsepra age: 21.59 43.98 97.8 1.4 6.44 1.10 Range: Low High 16.83 29.75 _-- 10905..03 5.26 8.43 * UDS = Average of net nuclear grain counts + standard deviation EP from tripli- ** Acvaetreagoer dvaulpuleiscatfeorctovreirpslliicpaste(o1r50ducpellilsc)ateancaolvyezresdlifposr aforsinaglseingalneimaaln.imal. a SD = Standard Deviation 15516-0-494 31 01322 g WASHINGTON HISTORICAL POSITIVE CONTROLS IN VIVO/IN VITRO UNSCHEDULED DNA SYNTHESIS ASSAY 15-Hour Timepoint Number of data points is 12 Animal # DNuScleGursai5nsD/ * %NetofNNuucclleeair wGirtahins25++ AGvreariangse**Cyto 21 1123..6758 12..5320 34 172..7273 12..7834 65 98..2867 11..1155 7 9.14 1.48 8 9 65..0616 21..7909 1110 1101..1052 21..1137 12 15.40 1.07 7860..77 69..0954 7662..70 75..7718 7 6696..40 55..050 80.7 a 5406..00 22..5713 6781..73 76..0195 84.7 5.61 Average: 10.16 sRpaange: 2.99 HLiogwh 155..4606 1629..04 25..0669 580..70 92.H4 * UDS = Average of net nuclear grain counts + standard deviation frostripli*x Acavteeragoer vdaulpuleiscatfeorcotvreirpslliicpaste(o15r0ducpelllisc)ateancaolvyezresdlifposr aforsiangsliengalniadnli.mal a SD = Standard Deviation 15516-0-494 & coL324