LC Labs/R-3692 Rociletinib, Free Base, >99%/R-3692/500 mg

• Rociletinib,alsoknownasCO-1686,isanirreversIBLetyrosinekinaseinhibitorwithaKiof21.5nMfortheEGFRL858R/T790MmutantandaKiof303.3nMforwtEGFR.Itinhibitedthegrowthofnon-smallcelllungcancer(NSCLC)cellsexpressingmutantEGFR,anditinducedapoptosis.Italsodemonstratedinvivoanti-tumoractivityinmicebearingNSCLCtumorswithactivatingEGFRmutations.WalterA.O.,etal."Discoveryofamutant-selectivecovalentinhibitorofEGFRthatovercomesT790M-mediatedresistanceinNSCLC."CancerDiscov.3:1404-1415(2013).
• TheT790MmutationisthemostcommonreasonforacquiredresistancetoexistingEGFRinhibitorsinNSCLC.RociletinibpotentlyinhibitedmutantEGFRL858R/T790MwithanIC50< 0.51nM. Rociletinib blocked the growth of T790M-positive NSCLC cells in vitro and in vivo. Walter A.O., et al. "CO-1686, a novel mutant-selective EGFR inhibitor, overcomes T790M mediated resistance in non-small cell lung cancer (NSCLC)." http://www.clovisoncology.com/assets/pdf/CO-1686/Clovis-Avila_AACR_2012_CO-1686_Poster_ClovisFINAL_27MAR12.pdf
• AphaseIclinicaltrialinpatientswithEGFRmutatedNSCLCdemonstratedthatrociletinibwaswelltolerated,andactivitywasobservedindoseescalationcohorts.SequistL.V.,etal."First-in-humanevaluationofCO-1686,anirreversible,selective,andpotenttyrosinekinaseinhibitorofEGFRT790M."http://www.clovisoncology.com/files/CLVS_ASCO_2013_poster_CO1686_P1monotx_abstract2524.pdf
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,veterinary,food,orhouseholduse
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.