Erlotinib

E-4007Erlotinib,HydrochlorideSalt,>99%[CP-358774][OSI-774][Tarceva]M.W.429.90C22H23N3O4•HCl[183319-69-9]M.I.14: 3672Storage: Storeatorbelow-20ºC. Solubility: SolubleinDMSOat18mg/mLwithwarming;verypoorlysolubleinethanol;verypoorlysolubleinwater;maximumsolubilityinplainwaterisestimatedtobeabout5-20µM;buffers,serum,orotheradditivesmayincreaseordecreasetheaqueoussolubility. Disposal: A•Inhibitoroftheepidermalgrowthfactorreceptortyrosinekinase,whichishighlyexpressedandoccasionallymutatedinvariousformsofcancer. ErlotinibbindsreversIBLytotheATPbindingsiteofthereceptor. Raymond,E.,etal. "Epidermalgrowthfactorreceptortyrosinekinaseasatargetforanticancertherapy." Drugs60Suppl1: 15-23,discussion41-42(2000).•ErlotinibisaninhibitorofhumanEGFRtyrosinekinase(IC50=2nM)anddecreasesEGFRautophosphorylationintumorcells(IC50=20nM). Moyer,J.D.,etal. "InductionofApoptosisandCellCycleArrestbyerlotinib,anInhibitorofEpidermalGrowthFactorReceptorTyrosineKinase." CancerRes.57: 4838-4848(1997).•ErlotinibhasbeenshowntobeapotentinhibitorofJAK2-V617F,amutantoftyrosinekinaseJAK2foundinasubstantialproportionofpatientswithidiopathicmyelofibrosisoressentialthrombocythemiaandmostpatientswithpolycythemiavera(PV). ThestudyindicatesthaterlotinibmaybeusedtotreatJAK2-V617F-positivePVandothermyeloproliferativedisorders. Li,Z.,etal."ErlotinibeffectivelyinhibitsJAK2V617Factivityandpolycythemiaveracellgrowth." J.Biol.Chem.282: 3428-3432(2007).•FoundtobeapotentinhibitorofEGFRkinase(Ki=0.7nM),butmuchweakerforErbB-2kinase(Ki=1µM)andErbB-4kinase(Ki=1.5µM). Wood,E.R.,etal. "AUniqueStructureforEpidermalGrowthFactorReceptorBoundtoGW572016(Lapatinib),RelationshipsamongProteinConformation,InhibitorOff-Rate,andReceptorActivityinTumorCells." CancerRes.64: 6652-6659(2004).•ErlotinibistheactiveingredientinthedrugsoldunderthetradenameTarceva®. Thisdrughasbeenapprovedinatleastonecountryforuseinpatientswithpancreaticcancer,non-smallcelllungcancerandseveralothertypesofcancer. NOTE: THEERLOTINIB,HYDROCHLORIDESALTRESEARCHCOMPOUNDSOLDBYLCLaboratoriesISNOTTARCEVA®,ANDISNOTFORHUMANUSE.•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.