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Bpsbioscience/AT13387/27736-1/5 mg

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MW:409.5DaCASRegistry#:912999-49-6Formula:C24H31N3O3Target:HSP90Description:AT13387,discoveredbyahigh-throughputx-raycraystallographyfragment-basedplatform,isanon-geldanamycininhibitorofheatshockproterin90(HPS90),amoleculechaperoneregulatingsignaltransductionpathwaysforcellgrowthandsurvival.IthashighaffinityforbindingHSP90(Kd=0.5nM)andexhibitedaninvitrocytotoxicityshowingamedianEC50valueof41nM.TheantitumoractivityofAT13387againstsolidtumorandleukemiamodelsissimilartoalvespimycin.Synonym(s):(2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanoneBIOLOGicalActivity:AT13387isapotentinhibitoroftheproliferationandsurvivalofmanydifferentcelllines(suchasMES-SAcellline)fromavarietyofdifferenttumortypes.Acrossapanelof30tumorcelllines,AT13387potentlyinhibitscellproliferationwithGI50valuesintherange13-260nM.AT13387inhibitsproliferationofthenon-tumOrigenichumanprostateepithelialcelllinePNT2withaGI50valueof480nM.TheinhibitionofanumberofisolatedkinasesbyAT13387isalsoinvestigatedincludingCDK1,CDK2,CDK4,FGFR3,PKB-b,JAK2,VEGFR2,PDGFRβandAuroraB.Noneofthetestedkinasesaresignificantlyinhibitedatconcentrationsbelow30µM.Solubility:SolubleinDMSOStorage/StABIlity:Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.Reference(s):MinH.etal.PediatrBloodCancer.2012;59(1):185-188.ScientificCategory:HSPInhibitorProductType:InhibitorDatashownislot-specific.Contactusforspecificinformationonotherlots.

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