LC Labs/S4680 Sonidegib, Free Base, >99%/S4680/10 mg

Sonidegib,alsoknownasNPV-LDE-225andLDE-225,isapotentandselectivesmoothened(Smo)antagonist.Itinhibitedtheactivationofhedgehogsignaling,stimulatedwith1nMand25nMAg1.5,withIC50valuesof0.6and8nM,respectively.ItinhibitedSmobindingwithIC50valuesof1.3nMformouseSmoand2.5nMforhumanSmo.SonidegibdemonstratedinvivoantitumoractivityinsubcutaneousandorthotopicPtch+/-p53-/-medulloblastomaallograftmodels.PanS.,etal."DiscoveryofNVP-LDE225,aPotentandSelectiveSmoothenedAntagonist."ACSMed.Chem.Lett.1:130–134(2010).
Thisresearchcompoundisthefreebaseformofsonidegib.Wealsoofferthediphosphatesaltform;pleaseseeSonidegib,DiphosphateSalt,Cat.No.[S-4699]
TreatmentwithsonidegibinhibitedtheHedgehog-GLIpathway,inducedG1cellcyclearrest,andresultedindecreasedviabilityandinductionofapoptosisinhumanmelanomacelllinesinvitro.ItdemonstratedantitumoractivityagainsthumanmelanomaandreducedGLI1expressioninvivo.JaliliA.,etal."NVP-LDE225,apotentandselectiveSMOOTHENEDantagonistreducesmelanomagrowthinvitroandinvivo."PLoSOne8:e69064(2013).
AdditionofthePI3KinhibitorNVP-BKM120orthedualPI3K-mTOR(mammaliantargetofrapamycin)inhibitorNVP-BEZ235totheinitialtreatmentofmedulloblastomawithsonidegibmarkedlydelayedthedevelopmentofresistancetosonidegibinmice.BuonamiciS.,etal."InterferingwithresistancetosmoothenedantagonistsbyinhibitionofthePI3Kpathwayinmedulloblastoma."Sci.Transl.Med.2:51ra70(2010).
Sonidegibinhibitedepithelial-mesenchymaltransitionandhumanprostatecancerstemcellgrowth.NantaR.,etal."NVP-LDE-225(Erismodegib)inhibitsepithelial-mesenchymaltransitionandhumanprostatecancerstemcellgrowthinNOD/SCIDIL2RγnullmicebyregulatingBmi-1andmicroRNA-128."Oncogenesis2:e42(2013).
Sonidegibinhibitedmelanomacellgrowthinvitroandinvivo.OReillyK.E.,etal."Hedgehogpathwayblockadeinhibitsmelanomacellgrowthinvitroandinvivo."Pharmaceuticals(Basel)6:1429-1450(2013).
Thissonidegibproductisthefreebaseform,whoseCASnumberisgivenabove.TheCASnumberofthediphosphatesaltformis1218778-77-8.
AnotherCASnumberpreviouslyassignedtoSonidegib,FreeBase,namely1270169-93-1,hasbeendeletedbyCASandisnolongerinuse.
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.

M.W.485.50
C26H26F3N3O3
[956697-53-3]

对照品标准品，生物试剂盒，gibco胎牛血清，试剂采购网，中国试剂网，细胞因子试剂盒

LC Labs/S4680 Sonidegib, Free Base, >99%/S4680/10 mg