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SRPT T-7& J MIN 314l022208 PERJ%UOROO~AlVE2WLFONYLFLUORIDE T-7 b ,OSF) t .a BACTERJAL REVERSE MUTATION TEST Sponsor 3M Center 3M Corporate Toxicology Building 220-2E-02 St Paul I"55133-3220 USA Research Laboratory HuntingdonLife SciencesLtd. Woolley Road Alconbury Huntingdon Cambridgeshire PE28 4HS ENGLAND Report issued 23 October 2002 Page 1 of 29 001570 . . ..................... MIN 3141022208 CONTENTS Page COMPLIANCE WITH GOOD LABORATORYPRACTICE STANDARDS ............................. 3 QUALITY ASSURANCE STATEMENT ..................................................................................... 4 RESPONSIBLE PERSONNEL ...................................................................................................... 5 SUMMARY ................................................................................................................................... 6 INTRODUCTION .......................................................................................................................... 7 TEST SUBSTANCE ...................................................................................................................... 9 EXPERIMENTALPROCEDURE ................................................................................................ 10 ASSESSMENT OF RESULTS ...................................................................................................... 14 DEVIATIONS FROM PROTOCOL .............................................................................................. 14 MAINTENANCEOF RECORDS ................................................................................................. 15 RESULTS ....................................................................................................................................... 16 CONCLUSION .............................................................................................................................. 16 REFERENCES ............................................................................................................................... 17 TABLES 1. Results obtained with S. typhimuriumTA98: test 1 (range-finding) ..................................... 18 2. Results obtained with S. typhimurium TA98: test 2, with pre-incubation ............................. 19 3. Results obtained with S. typhimuriumTAIOO: test 1 (range-finding).................................... 20 4. Results obtained with S.typhimuriumTAI00:test 2, with pre-incubation ........................... 21 5. Results obtained with S.typhimuriumTA1535: test 1 (range-finding).................................. 22 6. Results obtained with S. typhimurium TA1535: test 2, with pre-incubation ......................... 23 7. Results obtained with S. typhimuriumTA1537: test 1(range-finding).................................. 24 8. Results obtained with S. typhimuriumTA1537: test 2, with pre-incubation ......................... 25 9. Results obtained with E. coli WP2mA/pKh4101 (CM891): test 1 (range-finding).............. 26 10. Results obtained with E. coli WP2uvrA/pKh4101(CM891):test 2, with pre-incubation ..... 27 APPENDICES 1. Historicalcontrol data ............................................................................................................. 28 2. Eye Research Centre GLP ComplianceStatement2001 ........................................................ 29 2: MIN 3 141022208 COMPLIANCE WITH GOQD LABORATORY PRACIlCE STANDGRDS The study described in this report was conducted in compliance with the following Good Laboratory Practice Standards, with the exceptionsstated below, and I considerthe data generated to be valid. The UK Good Laboratory Practice Regulations 1999 (Statutory Instrument No. 3106). EC Commission Directive 1999111EC of 8 March 1999(Official Journal No. L 77/8). OECD Principles of Good Laboratory Practice (as revised in 1997), ENV/MC/CHEM(98)17. In line with normal practice in this type of short-term study, the protocol did not require analysis of the dose form. The expiry date of the test sample was the Sponsor's responsibility. eR/Q ............tz,....................... 9.......... Kenneth May, B.Sc.,C.Biol., lkf.Biol., Study Director, Huntingdon Life SciencesLtd. .2..3..........O.....c....k....O....llb....c.. .l..r...f..mL Date :3: -- . . . _- _ _ -. . . . . ....... ..... MIN 314/022208 QUALITY ASSURANCE STATEMENT The following inspectionsand audits have been b e d out in relation to this study: Study Phase Protocol Audit Process Based Inspections S9 Preparation Formulation and Treatment Plate Scoring Report Audit Date of Inspection 16 October 200 1 15 January 2002 31 October 2001 24 October 2001 4 February 2002 Date of Reporting 16 October 2001 15 January 2002 31 October 2001 24 October 2001 5 February 2002 Protocol Audit: An audit of the protocol for this study was conducted and reported to the Study Director and Company Managementas indicated above. Process Based Inspections: At or about the time this study was in progress inspections of routine and repetitive procedures employed on this type of study were carried out. These were conducted and reported to appropriateCompany Managementas indicated above. Report Audit: This report has been audited by the Quality Assurance Department. This audit was conducted and reported to the Study Director and Company Managementas indicated above. The methods, procedures and observations were found to be accurately described and the reported results of this study to reflect the raw data. &"".""h"'r;" 4.....f....e........*.........3.....J........................ Angela Myennings, B.Sc., MSc., Ph.D., M.R.Q.A., Date Group Manager, Department of Quality Assurance, Huntingdon Life Sciences Ltd. 001573 :4: RESPONSIBLE PERSONNEL Kenneth May, B.Sc., C.Biol.,M.J.Bio1. Study Director Elizabeth Farrall, B.Sc. Scientist MM 3 141022208 001574 :5: MIN 3141022208 SUMMARY In this in viiro assessment of the mutagenic potential of Perfluorooctanesulfonyl fluoride (POSF), histidine dependent auxotrophic mutants of Salmonella typhimurium, strains TA1535,TA1537,TA98 and TA100, and a tryptophan dependent mutant of Escherichia coli, strain wP2uvrNpKM101 (CM89l), were exposedto the test substance. Two independentmutation tests were performed in the presence and absence of liver preparationsfrom Aroclor 1254induced rats (S9 mix). Both tests involved a pre-incubation stage in airtightvessels. Concentrations of Perfluorooctanesulfonyl fluoride (POSF)up to 5000 pglplate were tested in the mutation tests. This is the standard limit concentration recommended in the regulatory guidelines that this assay follows. No signs of toxicity were observed towards the tester strains in either mutation test. No evidence of mutagenic activity was seen at any concentration of Perfluorooctanesulfonyl fluoride (POSF)in either mutationtest. The concurrent positive controls demonstratedthe sensitivityof the assay and the metabolising activity of the liver preparations. It is concluded that, under the test conditions employed, Perfluomtanesulfonyl fluoride (POSF) showed no evidence of mutagenic activity in this bacterial system. 001575 :6: MIN 3 14/022208 INTRODUCTION This report describes a study designed to assess the mutagenic potential of Pedluorooctanesulfonyl fluoride POSF) in a bacterial system. The study was conducted in compliance with the following guidelines: OECD Guidelines for the Testing of Chemicals. (1997) Genetic Toxicology: Bacterial Reverse Mutation Test, Guideline471. EC Commission Directive 2000/32/EC Annex 4D-B.13/14. Mutagenicity - Reverse mutation test in bacteria. No. L 136/57. US EPA (1998) Health Effects Test Guidelines. OPPTS 870.5100 Bacterial reverse mutation test. EPA 712-C-98-247. Japan Ministry of Agriculture, Forestry and Fisheries. (1985) Notification of Director General, Agricultural Production Bureau. NohSan No. 4200. Joint Directives of J EPA, J M H W and J MITI. (31 October 1997) Kanpoan No. 287, Eisei No. 127 and Kikyoku No. 2 (31 October 1997). JMHW Genotoxicity Testing Guideline, PAB Notification No. 1604 (1 November 1999). Official Notice of J MOL. (8 February 1999). The method described was also designed to comply with ICH (1995 & 1997), and followed the recommendationsof the United Kingdom Environmental Mutagen Society (Gatehouse et all990). The in vitro technique described by Ames and his co-workers (Ames, McCann and Yamasaki 1975, Maron and Ames 1983) enables the mutagenic effect of a test substance to be determined by exposing specially selected strains of Salmonella typhimurium to the test substance. Normally S.typhimuriumis capable of synthesising the essential amino acid, histidine, but the mutant strains used in this test are incapable of this function. When these strains are exposed to a mutagen, reverse mutation to the original histidine independentform takes place in a proportion of the population. These are referred to as revertants, and are readily detected by their ability to grow and form colonies on a histidine deficient medium (supplemented with biotin, since these strains are also incapable of biotin synthesis). A techniquebased on similar principleshas also been described by Green (1984). This system employs mutant strains of Escherichiacoli that are incapable of synthesisingthe amino acid, tryptophan, which is required for growth. The strains used cany additional mutations that render them more sensitive to mutagens. The S.typhimurium strains have a defective cell coat, which allows greater permeability of test substances into the cell. All the strains are deficient in normal DNA repair processes. In addition, three of them possess a plasmid (pKh4101), which introduces an error-prone repair process, resulting in increased sensitivityto some mutagens. 001576 :7: MM 3 141022208 Many substances do not exert a mutagenic effect until they have been metabolised by enzyme systems not available in the bacterial cell. Therefore, the bacteria and test substance are incubated in both the absence and presence of a supplemented liver hction (S9 mix) prepared from rats previously treated with a substance (Aroclor 1254) known to induce a high level of enzyme activity. The protocol was approved by Huntingdon Life SciencesManagementon 18 July 2001, by the Sponsor on 31 July 2001 and by the Study Director on 15 October 2001. The study was conducted at Huntingdon Life Sciences Ltd., Eye Research Centre, Eye, Suffolk, IP23 7PX, England. Experimental start date: 21 November 2001. Experimentalcompletiondate: 31January 2002. 001577 . . Identity: Appearance: Storage conditions: Lot number: Expiry date: Purity: Specific gravity: Date received: MM 3 141022208 TEST SUBSTANCE Perfluorooctanesulfonylfluoride (POSF) Clear liquid Room temperature 040227 Sponsor'sresponsibility;assumed stable for duration of study ca 1.8 14 June 2001 001578 EXPERIMENTAL PROCEDURE MIN 314l022208 BACTERIALSTRAINS The following strains were used: S.typhimurium TA1535: contains a histidine missensemutation (hFFG46) but is also deficient in a DNA repair system (WB) and has a defective lipopolysaccharide coat on the cell wall ($I mutation). It is reverted by many agents causing base-pair substitutions,but is not sensitiveto frameshiftmutagens. S.fyphimuriumTAIOO: is the same as TA1535 but contains a resistance transfer factor conferring ampicillin resistance and increasing sensitivity to some mutagens (plasmid pKMI01). In addition to base-pair substitutions, it is also able to detect certain frameshift mutagens. S. typhimurium TA1537: bears a histidine frameshift mutation (hisC3076). Like TA1535, it is defective in a DNA repair system and lipopolysaccharide coat. It is sensitive to agents causing frameshift mutations involving insertion or deletion of a single base-pair. S.typhimurium TA98: contains another histidine frameshift mutation (hisD3052). Again it has a defective DNA repair system and lipopolysaccharide coat but also contains the pKMlOl plasmid. It is reverted by agents causing deletion of two adjacent base-pairs (double frameshift mutations), but not by simple alkylatingagents causing base-pair substitutions. E. coli W u v r A l p K M 101: (CM891) contains an ochre mutation. It is reverted by many agents causing A-T base-pair substitutions at the trpE locus or by G-C base-pair substitutions in transfer RNA loci elsewhere in the chromosome. It is also deficient in a DNA repair system (uvrA), and is more readily reverted by certain mutagens than its parent strain WP2. It also contains the pKM101 plasmid. The strains of S.typhimuriumwere obtained from the National Collection of Type Cultures, London, England. The Strain of E. coli was obtained from the National Collections of Industrial and Marine Bacteria, Aberdeen, Scotland. Batches of the strains were obtained fkom master stocks held in liquid nitrogen. The test batches were aliquots of nutrient broth cultures and were stored at -8OOC. Dimethyl sulphoxide (DMSO) was added to the cultures at 8% vlv as a cryopreservative. Each batch of frozen strain was tested, where applicable, for cell membrane permeability (rfa mutation), sensitivity to W light and the pKMlOl plasmid, which confers resistance to ampicillin. The responses of the strains to a series of diagnostic mutagens were also assessed. For use in tests, an aliquot of frozen culture was added to 25 ml of nutrient broth and incubated, with shaking, at 37C for 10 hours. These cultureswere intended to provide approximately lo9cells per ml, which were measured by spreadingaliquots (0.1 ml) of a dilution of the overnight cultures on the surface of plates of nutrient agar and counting the resultant colonies. 001579 - _. -- MIN 3141022208 POSITTVE CONTROLS In the absence of S9 mix Identity: CASNo.: Supplier: Lot number: purity: Appearance: Solvent: Concentration: Identity: CASNo.: Supplier: Lot number: Purity: Appearance: Solvent: concentration: Identity: CASNo.: Supplier: Lot number: Purity: Appearance: Solvent: Concentration: Identity: CASNo.: Supplier: Lot number: Purity: Appearance: Solvent: Concentration: In the presence of S9 mix Identity: CASNo.: Supplier: Lot number: Purity: Appearance: Solvent: Concentration: Sodium a i d e 26628-22-8 Sigma Chemical T7H0079 min. 99.5% White powder DMSO (Aldrich, A.C.S. spectrophotometricgrade) 0.5 clglplate for strains TA1535 and TAlOO 9-Aminoacridine 90-45-9 Sigma Chemical 1O6F-0668 1 > 97% Yellow powder DMSO (Aldrich,A.C.S. spectrophotometricgrade) 30 pglplate for strain TA1537 2-Nitrofluorene 607-57-8 Aldrich Chemical Company 80501-24227 98% Beige powder DMSO (Aldrich, A.C.S. spectrophotometricgrade) 1 pglplate for strain TA98 2-(2-Furyl)3-(5-nitro-2-furyl) acrylamide (AF-2) 3688-53-7 Wako Pure Chemical Industries Ltd. PAE 1151 98-102% Red powder DMSO (Aldrich, A.C.S. spectrophotometricgrade) 0.05 pglplate for strain wP2uvrNpKM101 (CM891) 2-Aminoanthracene 613-13-8 Aldrich Chemical Company 52234-024 96% Green powder DMSO (AIdrich, A.C.S. spectrophotometricgrade) 2 pdplate for strain TA1535 I0pglplate for strain WP2wA/pKMI 01 (CM891) : 11 001580 MTN 3141022208 Identity: CAS No.: Supplier: Lot number: Purity: Appearance: Solvent: Concentration: Benzo[a]pyrene 50-32-8 Aldrich Chemical Company 07778-105 98% Yellow powder DMSO (Aldrich,A.C.S. spectrophotometricgrade) 5 pg/plate for strains TA1537, TA98 and TAlOO PREPARATIONOF S9 FRACTION Species: Sex: Strain: source: Weight: Rat Male Sprague-Dawley derived Charles River UK Ltd. 400g S9 fraction was prepared from a group of CLI I0 animals according to the method described by Ames, McCann and Yamasaki (1975). Mixed function oxidase systems in the rat livers were stimulated by Aroclor 1254, administered as a single intra-peritoneal injection in corn oil at a dosage of 500 mgkg body weight. On the fifth day after injection, following overnight fasting, the rats were killed by cervical dislocation and their livers asepticallyremoved. The following steps were carried out at 04OC under aseptic conditions. The livers were placed in 0.15M KCI (3 ml KCI : 1 g liver) before being transferred to a Potter-Elvehjem homogeniser. Following preparation, the homogenate was centrifuged at 9000 g for 10 minutes. The supernatant fraction (S9fraction) was dispensed into aliquots and stored at -8OOC or below. Each batch of S9 fraction was tested for sterilityand efficacy. Date of preparation: 17July 2001 (test I); 15January 2002 (test 2) PREPARATIONOF S9 MIX The S9 mix contained: S9 fraction (10% vh), MgCl, (8 mM), KCl(33 mM), sodium phosphate buffer pH 7.4 (100 mM), glucose-&phosphate (5 mM), NADPH (4 mM) and NADH (4 mM). All the cofactors were filter-sterilised before use. FORMULATION OF TEST SUBSTANCE The solubilityof the test substancewas assessed in dimethyl sulphoxide(DMSO), ethanol, acetone and heme. It was insoluble in DMSO, ethanol and acetone, and was known to be insoluble in water. Although soluble in h e m e at 50 mglml, the volume of h e m e required to administerthe test substance at this concentration was found to be too toxic towards the test system. It was, therefore., decided to administerthe test substanceby direct addition withoutthe use of a solvent All concentrations cited in this report are expressed in terms of the Perfluorooctanesulfonylfluoride (POSF) sample as received. : 12: MIN 3 14/022208 MUTATION TEST PROCEDURE First test (range-finding) The testsubstancewas added to cultures of the five tester strains at seven concentrations. The highest concentration of test substance tested was 5000 Clglplate (obtained by addition of 2.8 pl of the test substance). This is the standard limit concentration recommended in the regulatory guidelines this assay follows. The other concentrations were 2500 pdplate (1.4 pl), 1750 pgplate (1.0 pl), 1250 pglplate (0.7 pl), 700 pg/plate (0.4 pl), 350 ptglplate (0.2 pl) and 175 pglplate (0.1 pl). Untreated controlsand the appropriatepositivecontrolswere also included. Following the addition of the above aliquots of the test substance (or 0.1 ml of positive control solution) to airtight glass vessels, 0.5 ml S9 mix or 0.5 ml 0.1 M phosphate buffer (pH 7.4) was added,followed by 0.1 ml of a 10 hour bacterial culture. The mixtures were incubated at 37OC for 30 minutes with shaking before addition of 2 ml of agar containing histidine (0.5 mM) and tryptophan (0.5 mM). The mixtures were thoroughly shaken and overlaid onto previously prepared Petri dishes containing 25 ml minimal agar. Each Petri dish was individually labelled with a unique code correspondingto a sheet, identifying the contents of the dish. Three Petri dishes were used for each concentration. Plates were also prepared without the addition of bacteria in order to assess the sterility of the test substance, S9 mix and sodium phosphate buffer. All plates were incubated at 37OC for cu 72 hours. After this period the appearance of the background bacteria1 lawn was examined and revertant coloniescounted using a Domino automatedcolony counter. Any toxic effects of the test substance would be detected by a substantial reduction in revertant colony counts or by the absence of a complete background bacterial lawn. In the absence of any toxic effects the top concentration normally used in the second test would be the same as that used in the first. If toxic effects were observed a lower concentration might be chosen, ensuring that signs of bacterial inhibition are present at the top concentration. Ideally a minimum of three non-toxic concentrations should be obtained. If precipitate were observed on the plates at the end of the incubation period, at least four non-precipitating dose levels should be obtained, unless otherwise justified by the Study Director. Second test The second test was an exact repeat of the first test, except that only five concentrations were used. 5000 pgtplate was again chosen as the top concentration. STABILITYAND FORMULATION ANALYSIS The stability of the test substance and the stability and homogeneity of the test substance in the test system were not detwmined as part of this study. Analysis of achieved concentration was not performed as part of this study. : 13: ASSESSMENT OF RESULTS Acceptance For a test to be considered valid the mean of the solventlvehiclecontrol revertant colony numbers for each strain should lie within the 99% confidence limits of the current historical control range of the laboratory unless otherwisejustified by the Study Director. The historical range will be maintained as a rolling record over a maximum of five years. Also, the positive control compounds must cause at least a doubling of mean revertant colony numbers over the negative control. Analysis The mean number of revertant colonies for all treatment groups will be compared with those obtained for the solvent/vehicle control groups. Evaluation If exposure to a test substance produces an increase in revertant colony numbers of at least twice the concurrent solventlvehicle controls, with some evidence of a positive dose-relationship (increased revertant colony counts at concentrations below that at which the maximal increase is obtained), in two separate experiments, with any bacterial strain either in the presence or absence of S9 mix, it will be considered to show evidence of mutagenic activity in this test system. No statistical analysis will be perfonned. If exposure to a test substance does not produce an increase in revertant colony numbers in two separate experiments, with any bacterial strain either in the presence or absence of S9 mix, it will be consideredto show no evidence of mutagenic activity in this test system. No statistical analysis will be performed. If the results obtained fail to satisfy the criteria for a clear "positive" or "negative" response, even after the additional testing outlined in the mutation test procedure, the test data may be subjected to analysis to determine the statistical significance of any increases in revertant colony numbers. The statistical procedures used will be those described by Mahon et aZ(1989) and will usually be analysis of variance followed by Dunnett's test. Biological significance should always be considered along with statistical significance. It should be noted that it is acceptable to conclude an equivocal response if no clear results can be obtained. DEVIATIONS FROM PROTOCOL Although the protocol indicated that a solvent or vehicle would be employed, it was not possible to obtain a solution or suspension of the test substance that would be compatible with the test system. The test substance was, therefore, added directly to the test system. Since this procedure complies with the test guidelines that this study follows, this deviation does not impact on the integrity of the study. 001583 14 : MIN 3 141022208 MAINTENANCE OF RECORDS All raw data, samples and specimens (if appropriate) arising fiom the performance of this study will remain the property of the Sponsor. Types of sample and specimen which are unsuitable, by reason of instability, for long term retention and archiving may be disposed of after the periods stated in Huntingdon Life Sciences Standard OperatingProcedures. All other samples and specimens and all raw data will be retained by Huntingdon Life Sciences in its archive for a period of five years from the date on which the Study Director signs the finai report. After such time, the Sponsorwill be contacted and his advice soughton the return, disposal or further retention of the materials. If requested, Huntingdon Life Sciences will continue to retain the materials subjectto a reasonablefee being agreed with the Sponsor. Huntingdon Life Sciences will retain the Quality Assurance records relevant to this study and a copy of the final report in its archive indefmitely. 001584 MIN 3 14l022208 RESULTS The results obtained with Peffluorooctanesulfonylfluoride (POSF) and positive control compounds are presented in Tables 1 to 10. The mean values quoted have been corrected to the nearest whole number. The absence of colonies on sterilitycheck plates confmed the absence of microbial contamination. The total colony counts on nutrient agar plates (see Tables) confinned the viability and high cell density of the cultures of the individual organisms. The mean revertant colony counts for the solvent controls were within the 99% cofidence limits of the current historical control range of the laboratory. Appropriate positive control chemicals (with S9 mix where required) induced substantial increases in revertant colony numbers with all strains, confuming sensitivityof the cultures and activityof the S9 mix. FIRST TEST (RANGE-FINDING) No substantial increases in revertant colony numbers over control counts were obtained with any of the tester strains following exposure to Peffluorooctanesulfonylfluoride (POSF) at any concentration .in either the presence or absenceof S9 mix. No visible thinning of the background lawn of non-revertant cells was obtained following exposure to Perfluorooctanesulfonyl fluoride (POSF). A maximum exposure concentration of 5000 pg/plate was, therefore, selected for use in the second test. SECOND TEST No substantial increases in revertant colony numbers over control counts were obtained with any of the tester strains following exposure to Perfluorooctanesulfonylfluoride (POSF) at any concentration in either the presence or absence of S9 mix. No visible thinning of the background lawn of non-revertant cells was obtained following exposure to Perfluorooctanesulfonylfluoride(POSF). CONCLUSION It is concluded that, under the test conditions employed, Perfluomtanesulfonyl fluoride (POSF) showed no evidenceof mutagenicactivity in thisbacterial system. MM 3 141022208 REFERENCES A M E S , B.N., McCA", J. and YAMASAKI, E. (1975) Methods for detecting carcinogens and mutagens with the Salmonellafmammalianmicrosomemutagenicity test. Mutation Res. 31,347-364. GATEHOUSE, D.G., ROWLAND, LR, WILCOX, P., CALLANDER,RD. and FORSTER,R (1990) Bacterial mutation assays in: KIRKLAND, D.J. (Ed.). WMS Sub-committee on Guidelines for Miuagenicity Testing. Report. Part I revised Basic Murageniciq Tests: UKElUY Recommended Procedwes, pp.13-61.CambridgeUniversityPress,Cambridge. GREEN, M.H.L. (1984)Mutagen testing using trp+ reversion in Escherichia coli in KILBEY, B.J., LEGATOR, M., NICHOLS, W.and RAMEL, C. (Eds.). Handbook of Mutagenicity Test Procedures. Secondedition, pp.161-187.Elsevier SciencePublishersBV,Amsterdam. ICH(1 995) Genotoxicity: Guidance on SpecificAspects of Regulatory GenotoxicityTests. ICH (1997)Genotoxicity: A StandardBattery of GenotoxicityTesting of Pharmaceuticals. MAHON, G.A.T., GREEN, M.H.L., MIDDLETON, B., MITCHELL, I.de G., ROBINSON, W.D.and TWEATS, DJ. (1989)Analysis of data from microbial colony assays in: Kw(LAND, D.J. (Ed.). UKEUSSub-committeeon Guidelinesfor Miitagenicity Tmting.Report. Part DI. Statistical Evaluation of Mutageniciq TestData, pp.26-65. CambridgeUniversityPress,Cambridge. MARON, D.M. and AMES, B.N. (1983) Revised methods for the Salmonella mutagenicity test. Mutation Res. 113, 173-215. MJN 3 14/022208 TABLE 1 Results obtained with S.rypAimuriurn TA98:test 1 (rangefinding) I 'late No. Addition -1+ None; S9 mix sterility check 1 None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 POSF 9lPOSF 10 IUntrcated 11 POSF 12 POSF 13 POSF 14 POSF 15 POSF 16 POSF 17 POSF 18 Untreated 19 Benzo[a]pyrcnc 20 2-Nitrofluorene None; lo4 dilution of 21 overnight culture, plated on nutrient agar (5of3)Pg/Platt) (SO00 pg/plate) (2500 pg/plate) (1750 pg/platc) (1250 pg/platc) (700 pg/plate) (350 pg/plate) (175 pg/plate) (5000 puplate) (2500 pg/plate) 1750 pg/plate) 1250 &plate) (700Pg/Pl*) (350 pg/plate) (175 pdplate) (5 P d P W (1 Pg/PlaW -+Sp9remseknt absent + - + + + + + + + + - - - - + - r - I Revertant colony counts* and means B C Mkan sd 0 0 0 0 0 0 0 0 0 46 44 56 45 41 42 48 45 50 43 51 50 48 50 48 1 61 35 52 56 55 55 I 41 36 51 41 37 37 37 38 35 43 31 41 39 46 49 34 39 43 37 42 41 44 36 21 30 30 38 566 546 542 234 205 209 0 0 0 0 0 0 - 49 6 43 2 48 3 48 4 49 1 49 13 55 1 - 43 8 - 38 2 37 2 38 6 45 5 39 5 40 3 - 34 12 33 5 551 13 - - 216 16 133 I28 129 130 3 Except plate nos. 1,2 and 21 (total colony counts) sd Standard deviation 001587 : 18: . .- . ..- - .... ... TABLE 2 Results obtained with S. typhimuriumTA98: test 2 MIN 3 141022208 Plate Addition No. -14 None; S9 mix sterility chcck 1 . None; buffer sterility check A IPOSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 71POSF 8 Untrcatcd 9 POSF 10 POSF 11 POSF 12 POSF 13 FQSF 14 Untreated 15 Benzo[a]pyrene 16 2-Nitrofluorene None; 10" dilution of 17 overnight culture, plated on nutrient agar Revertant co S9 mix + present C - absent + 0 (5000 pglplate) - (50~Pg/PW + (2500 pglplatc) + (1750 pglplate) + 0 $ 0 39 36 43 36 (1250 pglplate) + 30 I I (700 &plate) + 51 42 46 I + 53 44 49 - I (5000 &plate) 21 39 34 - (25OoPdPlW 34 38 23 - (I750 pglplate) 37 35 35 - (1250 &plate) 29 31 29 - (700 pglplate) 32 38 23 38 39 31 (5 PglPlate) + 449 550 567 - (1 udolatel 504 467 443 - 1 1106 96 117 * Except plate nos. 1,2 and 17(totalcolony counts) sd Standard deviation Mean sd 0 0 0 0 0 0 43 5 38 3 40 3 36 7 46 I 5 49 5 31 9 32 8 36 I 30 1 31 8 36 4 522 64 471 31 106 11 : 19: TABLE 3 Results obtained with S. @phimnrium TA100: test 1 (range-finding) MN 3 141022208 IF1 Addition I+ None; S9 mix sterility check 1 - None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 POSF 9 POSF 10 Untreated 11 POSF 12 POSF 13 POSF 14 POSF 15 POSF 16 POSF 17 POSF 18 Unbeated 19 Benzo[a]pyrene 20 Sodium azidc None; lo* dilution of 21 overnightculture,plated I [onnutrient agar S9 mix + present - absent + (5000 &plate) - (SO00 pdplate) + (2500 pg/plate) + (1750 &plate) + (1250 pglplate) + (700 @plate) + (350 pglplatc) + (175 @plate) + + - (5000 &late) - (2500 &late) - (1750 pglplatc) - (1250 &plate) - ( 7 O o P d P W - P O P ~ / P W - (175 P d P W - (5 P d P W + (0.5 pglplate) * Except plate nos. 1,2and 21 (total colony count$ sd Standard deviation Revertmt colony counts* and means A B C Mean sd 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 125 169 137 148 130 152 153 164 154 159 141 165 154 131 114 159 145 131 143 159 128 148 140 131 119 131 122 125 132 88 125 121 139 88 118 124 138 97 136 119 118 125 122 122 109 112 110 141 573 507 568 360 453 47 1 144 23 143 12 157 6 155 12 133 20 145 14 143 16 140 9 124 6 115 24 128 9 110 19 124 23 121 4 118 8 121 17 549 37 428 60 :20 : TABLE 4 Results obtained with S. gphimurium TA100: test 2 MIN 3 14i022208 Plate Addition No. -1+ None; S9 mix sterility check 1 None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 Untreated 9 POSF 10 POSF 11 POSF 12 POSF 13 POSF 14 Untreated i 5 Benzo[a]pynne 16 Sodium azide None; lod dilution of 17 overnight culture, plated on nutrient agar S9 mix +present -absent + (5000~glPW - (5000 pglplate) + (Z00Pg/PW + (1750 &plate) + (1250 pglplatc) + (700 pdplate) + (5000 pglplate) +- - (2500 pglplate) - (I 750 pglplate) - (1250 pglplate) - (700 pglplate) - (5 &plate) + (0.5 pglplate) Revermnt colony counts* and means ~ A B C Mean sd 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 131 I45 119 148 132 148 122 154 139 147 132 166 165 125 143 131 145 131 111 118 123 126 I37 121 135 128 147 119 128 124 150 124 125 143 123 122 752 706 705 528 50 1 549 132 13 143 9 138 16 148 17 144 20 136 8 117 6 128 8 137 10 124 5 133 15 129 12 721 27 526 24 109 110 111 110 1 * Except plate nos. 1,2 and 17(total colony counts) sd Standard deviation :21: MTN 3 14l022208 TABLE 5 Results obtained with S.@phimurium TA1535: test 1(range-finding) 'I& Addition No. -1+ None; S9mix sterility theck 1 None;buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 POSF 9 POSF 10 Untreated 1 1 POSF 12 POSF 13 POSF 14 POSF I5 POSF 16 POSF 17 POSF 18 Untreated 19 2-Aminoanthraccne 20 Sodium s i d e None; lod dilution of 21 overnight culture, plated on nutrient agar (5OoOWpl-1 S9 mix +present - absent + - (~O~OP~/PW+ (2500pglplate) + (1750pglplate) + (1250pg/plate) + (700 @plate) + (350pglplate) + (1 75 pg/plate) + + (5000pg/plat~) - (2500pg/plate) - - (I750pdplate) - (1250pg/plate) (700 &plate) - - (350pg/plate) - (175 pg/plate) (2P g / P W + (0.5pg/plate) - Except plate nos. 1.2 and 21 (total colony counts) sd Standard deviation Revertant colony counts* and means I I - - A B C MlXll sd - - 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 - 14 21 16 17 4 20 26 16 21 5 29 22 12 21 9 14 26 20 20 6 22 23 19 21 2 17 23 20 20 3 14 20 19 18 3 - - 31 28 19 26 6 - - 21 I5 22 19 4 15 19 14 16 3 20 14 24 19 5 17 15 21 I8 3 19 16 24 20 4 16 I5 19 17 2 21 20 20 - 22 20 21 - - 282 324 247 - - 231 252 25 1 20 1 21 I 284 39 245 12 184 165 175 175 10 - - 001591 : 22 : . ... TABLE 6 Results obtained with S. rypirimurtkm TAI535: test 2 MIN 3 141022208 Addition No. 1+ None; S9 mix sterility check 1 - None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 Untreated 9 POSF 10 POSF 11 POSF 12 POSF 13 POSF 141Untreated 15 2-Aminoanthracene 16 Sodium azide None; lod dilution of 17 overnight culture, plated on nutrient agar S9 mix +present - absent + (5000 pglplate) - RI 'ertant wlonv counts* and means A 0 0 0 (5000PglPlW + 20 (2500 pglplate) + 19 (1750 pglplate) + 12 (1250 pglplate) + 20 (700 pglplate) + 21 + 22 - (5000 pglplate) 17 - (2500 pglplate) 15 - (1750 pglplate) 14 - (1250 pglplate) 21 - (700 pglplate) 22 27 (2 PglPlatC) + 145 (0.5 &plate) - 253 129 Except plate nos. 1,2 and 17 (total colony counts) sd Standard deviation : 23 : . TABLE 7 Resultsobtained with S. typhimurium TA1537:test 1 (range-finding) MIN 3 141022208 'late Addition VO. 1+ None; S9 mix sterility check I - None; buffer sterility check 2 WSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 POSF 9 POSF 10 Untreated 11 POSF 12 POSF 13 POSF 14 POSF 15 POSF 16 POSF 17 POSF ~ 18 Untreated 19 Benzo[a]pyrene 20 9-Aminoacridine None; 10" dilution of 21 overnight culture, plated on nutrient agar S9 mix -+present absent + (5000 bglplat~) - (5000 pglplate) + (2500 vglplate) + (1750 pglplate) + (I250 pdplate) + (700PdPW + (350 pdpiate) + (175 pglplate) + + - (5000 &plate) - (2500 pg/plate) - (I750 pg/plate) - (1250 pglplate) - (700 @plate) - (350 @plate) - (175 pg/plate) (5 P d P W + (30 pglplate) - Revertant colony counts* and means A B C Mean sd 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 23 22 15 26 22 16 23 27 21 21 27 19 21 22 26 26 21 24 17 24 24 22 22 26 19 15 10 15 10 13 17 17 10 17 19 10 16 16 12 13 9 15 13 13 10 16 15 13 355 394 360 489 457 453 20 4 21 5 24 3 22 4 23 3 24 3 22 4 23 2 1s 5 13 3 15 4 15 5 15 2 12 3 12 2 15 2 370 21 466 20 103 139 107 116 20 Except place nos. 1,2 and 21 (total colony counts) sd Standard deviation - 24 . TABLE 8 Results obtained with S. rypAimrrrium TA1537:test 2 MIN 3 141022208 'late Addition No. -1+ None; S9 mix sterility check 1 None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 Untreated 9 POSF 10 POSF 11 POSF 12 POSF 13 POSF 14 Untreated (5000 &plate) S9 mix -+ pnscnt absent + - (5000 pdplate) + (2500 pg/plate) + (1750 pglplatc) + (1250 pglplate) + (70OPglPW + + - (5000 pg/plate) - (2500 pdplate) -- ( 1 7 5 0 W ~ W (1250 pg/plate) (700FdPlW - None; lod dilutionof (30 P d P W on nutrient agar ~ Except plate nos. 1.2 and 17 (total colony counts) sd Standard deviation Revertant colony counts' 315 I 281 I 238 269 I 276 I 317 124 ' I 129 I 124 I0 13 4 12 2 14 I 3 -I 001594 : 25 : MIN 3 14fO22208 TABLE 9 Results obtained with El coli wpZUvrA/pKMlOl (CM891):test 1(range-finding) 'late Addition No. -I+ None; S9 mix sterilitycheck 1 None; buffer sterility check 2 POSF; sterility check 3 POSF 4 POSF 5 POSF 6 POSF 7 POSF 8 POSF 9 POSF 10 Untreated 11 POSF 12 POSF 13 POSF 14 POSF 15 POSF 16 POSF 17 POSF 18 Untreated 19 2-Aminoanthraccne 20 *-2+ None; lod dilution of 21 overnight culture, plated on nutrient agar S9 mix -+ present absent + (5000 &plate) - (5000~g/platc) + (2500 pglplate) + (1750 @plate) + (1250 pglplate) + (700 pglplate) + (350 pglplate) + (175 &plate) + + (5000 &plate) - - (=00Pg/Plate) - (1750 palate) - (I250 pglplate) - (700 P d P W - (350 pglplate) - (175 &plate) - (10 Pg/PlW + (0.05 &plate) Except plate nos. 1,2 and 21 (totalcolony counts) sd Standard deviation t 2-(2-Furyl)-3-(5-nitroro-t-furyl) acrylamidc -Revertant colc - Y counts* and met - A B C 0 0 0 0 0 0 0 0 0 107 131 87 119 136 96 126 122 116 123 96 119 122 144 123 122 138 119 117 121 119 123 121 133 101 112 99 111 82 89 132 118 116 85 138 85 110 86 110 95 74 84 -- 81 111 73 88 124 123 320 423 405 559 529 53 1 0 0 0 0 - - 0 0 108 22 117 20 121 5 113 15 130 12 I26 10 - - 119 2 126 6 104 7 94 15 122 9 103 31 102 14 84 11 - 88 20 112 21 - - - - 383 55 - 540 - 17 I62 188 217 189 28 - - :26 : MTN 3 14/022208 TABLE 10 Results obtained with B coli WP2uvrNpKM101 (CMS91): test 2 - Plate Addition No. -1t None;S9 mix sterility check 1. None; buffer sterility check 2 POSF; - sterility check 3 POSF 4 POSF < POSF f POSF 5 POSF -8 Untreated -5 POSF 1c POSF 11 POSF 12 POSF 13 POSF -14 Unecated -15 2-Aminoanthracene -16 AF-2+ -None; lod dilution of 17 overnight culture, plated on nutrient agar S9 mix -+present absent + (5CJOo Pg/Pbt4 - Rcvcrtant colony counts* and means A B C Mean sd 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 (50~Pg/PW + 125 136 122 128 7 (2500 pg/plate) + 154 122 165 147 22 (1750pg/plate) + 126 159 I45 143 17 (1250 pglplate) + 132 145 172 150 20 (700 pglplate) + + - (5000 pg/platc) - (2500 pg/plate) -- (1750 pg/plate) (1250 &late) - (700 pg/plat~) 184 143 166 137 144 165 147 148 128 121 139 155 144 131 145 13 1 13 1 139 115 110 135 164 21 149 I5 141 11 138 17 140 8 134 5 120 13 153 152 140 148 7 - (10 pglplatc) + 50 1 465 583 516 60 (0.05 pg/plate) 1041 899 957 966 71 190 175 189 185 8 Except plate nos. 1,2 and 17 (total colony counts) sd Standard deviation t 2-(2-Fury1>3-(5-nitro-2-furyl) acrylamide : 27 : MM 3 14/022208 ' APPENDIX1 Historical control data Presented below are the historical control data from the period 1 April 1997to 30 September2001. Untreated controls Strain S9 mix TAlOO - + TA1535 + wP2Wf NpKMl 01 (CM891) + TA98 - f TA1537 - + Minimum '78 81 12 10 79 73 23 29 7 7 Maximum 149 165 33 29 167 200 48 54 23 34 Meall 109 114 18 19 121 134 38 41 12 13 No.of values 309 313 307 311 214 218 311 315 308 312 Standard deviation 16 22 3 3 17 23 4 5 3 5 Upper 99% limit 151 168 33 29 170 204 49 55 23 35 Lower 99% limit 76 78 12 10 76 69 22 28 7 6 Positive controls Strain S9 mix TAlOO 4- Maximum 860 1327 1350 Mean 405 564 561 No. of values 346 441 808 Standarddeviation 120 175 189 TA1535 + 781 1130 1145 205 419 229 341 434 796 139 196 114 wP2uvrA/pKM101 - (CM891) -i. ( c ) ( e l (j) 294 244 188 2312 1533 1704 1331 679 659 112 415 549 488 183 250 TA98 TA1537 + 4- (f) (h) (g) (h) 123 123 39 67 993 1031 1933 543 320 517 350 246 788 810 569 810 115 165 337 80 (a) ENNG 3 pg @) m"N5 (c) m"N 2 Pg (d) Sodium azide OSpg (c) AF-2 0.05 pg (f)2-Nitrofluorme1 vg (g) 9-Aminoacridine 30 pg (h) Benzo[a]pyrene 5 pg (i) 2-Aminoanthraccne 2 pg (i) 2-Aminoanthracene 10 pg : 28 MIN 3 14/022208 APPENDIX 2 Eye Research Centre GLP ComplianceStatement2001 T H E D E P ~ O F H E A L T OBFTRE GOVERNMENT 0FTHEU"ITEDKINGDOM GOODLABORATORYPRACI'ICE LABORATORY BuntingdamLife S&ncrr Eye Reaurcb Centre Eye snffolk I n 3 7PX TESTTYPE '. -. DATE OF INSPECTION 29* January 2001 A general inspection for compliance with the Principles of Good Laboratory Practice was canied out at the above laboratory as part of UKGLP Compliance Programme. At the time of the inspection no deviuions were found of sufficient magnitude to affect the validity of non-clinical studies performedat tbae facilities. Dr.Roger G. Akxanda Head, UK GLPMonitoringAuthority OOlS98 29 :