LC Labs/I4122 Irinotecan, Hydrochloride Salt, Trihydrate, >99%/I4122/10 g

• Irinotecan(CPT-11)isatopoisomeraseIinhibitor.ItisasemisyntheticanalogofthenaturalalkaloidcamptothecinandhasanactivemetaboliteSN-38(7-Ethyl-10-hydroxycamptothecin).DuringtheSphaseofthecellcycle,camptothecinsselectivelybindtoandstabilizetopoisomeraseI-DNAcomplexes,inhibitingreligation,causingtheaccumulationoftopoisomeraseI-mediatedsingle-strandDNAbreaksintheDNA,andproducingirreversibledouble-strandDNAbreaksthatleadtocelldeath.Garcia-Carbonero,R.andSupko,J.G."Currentperspectivesontheclinicalexperience,pharmacology,andcontinueddevelopmentofthecamptothecins."Clin.CancerRes.8:641-661(2002).
• BothirinotecanandtopotecanhaveactivityinvivoagainstL1210andP388leukemia,mousecolonadenocarcinomas38and51,Lewislungcarcinoma,mousebreastadenocarcinoma16/C,andhumantumorxenograftsofB16melanomaandHT-29colonadenocarcinoma.Rothenberg,M.L."TopoisomeraseIinhibitors:Reviewandupdate."Ann.Oncol.8:837-855(1997).
• Inthehumantumorstemcellassay,irinotecanhasactivityinvitroagainstcolorectal,non-smallcelllung,ovarian,breast,mesothelioma,pancreas,sarcoma,andcervicalcancersatlowdrugconcentrations.Shimada,Y.,etal."ActivityofCPT-11(irinotecanhydrochloride),atopoisomeraseIinhibitor,againsthumantumourcolony-formingunits."AnticancerDrugs5:202-206(1994).
• Irinotecanisusedtotreatpatientswithcolorectalcancer.Fuchs,C.,etal."Irinotecaninthetreatmentofcolorectalcancer."CancerTreat.Rev.32:491-503(2006).
• IrinotecanisactivatedbyhydrolysistoitsactivemetaboliteSN-38.Kaneda,N.,etal."MetabolismandpharmacokineticsofthecamptothecinanalogueCPT-11inthemouse."CancerRes.50:1715-1720(1990).KawatoY.,etal."IntracellularrolesofSN-38,ametaboliteofthecamptothecinderivativeCPT-11,intheantitumoreffectofCPT-11."CancerRes.51:4187-4191(1991).
• SN-38isinactivatedbytheenzymeUGT1A1byglucuronidation.Iyer,L.,etal."Geneticpredispositiontothemetabolismofirinotecan(CPT-11).Roleofuridinediphosphateglucuronosyltransferaseisoform1A1intheglucuronidationofitsactivemetabolite(SN-38)inhumanlivermicrosomes."J.Clin.Invest.101:847-854(1998).
• IrinotecanistheactiveingredientinthedrugsoldunderthetradenameCamptosar®inUSAandCampto®inJapan.Thisdrughasbeenapprovedinatleastonecountryforuseinpatientswithmetastaticcolorectalcancer.NOTE:TheirinotecansoldbyLCLaboratoriesisNOTCamptosar®orCampto®,andisNOTforhumanuse.
• Watercontentmayvaryslightlyfromlottolot.Pleaserefertotheelementalanalysisofeachlotforthewatercontent.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanadianpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

RelatedTerms:

[Camptosar][Topotecin][Campto][Camptothecin11][CPT-11][U-101440E][DQ-2805]
M.W.677.18
C33H38N4O6•HCl•3H2O
[136572-09-3]
M.I.14:5091

Storage

Storeatorbelow-20ºC

Solubility

SolubleinDMSOat100mg/mL;verypoorlysolubleinethanol;solubleinwaterat25mg/mL;buffers,serum,orotheradditivesmayincreaseordecreasetheaqueoussolubility

Disposal

A