Flavopiridol-Hydrochloride-Alvocidib-Hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFlavopiridolHydrochlorideCat.No.:HY-10006CASNo.:131740-09-5Synonyms:AlvocidibHydrochloride;L86-8275Hydrochloride;HMR-1275Hydrochloride分⼦式:C₂₁H₂₁Cl₂NO₅分⼦量:438.3作⽤靶点:CDK;Autophagy;HIV作⽤通路:CellCycle/DNADamage;Autophagy;Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥20mg/mL(45.63mM)H2O:≥20mg/mL(45.63mM)DMF:7.69mg/mL(17.55mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2815mL11.4077mL22.8154mL5mM0.4563mL2.2815mL4.5631mL10mM0.2282mL1.1408mL2.2815mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.67mg/mL(1.53mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.67mg/mL(1.53mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FlavopiridolHydrochloride(AlvocidibHydrochloride)⼀种CDK的⼴谱抑制剂，与ATP竞争性地抑制CDK1，CDK2和CDK4的活性，IC50值分别为30,170,100nM。IC50&TargetCDK1/CycB1CDK2/CycECDK4/CycD1MAP30nM(IC50)170nM(IC50)100nM(IC50)19000nM(IC50)PKCEGFR14000nM(IC50)22000nM(IC50)体外研究Flavopiridol(2μM)robustlyinducesadistinctpatternofERstressinCLLcellsthatcontributestocelldeaththroughIRE1-mediatedactivationofASK1andpossiblydownstreamcaspases[1].FlavopiridolresultsinpotentupregulationofanumberofPRGsintreatmentslasting4-24h.Flavopiridolhasandimmediateandlong-termeffectontheexpressionofseveralPRGs.Inserumstarvedcellsre-stimulatedwithserum,flavopiridolalsoinhibitstheexpressionofthesegenes,butsubsequently,JUNB,GADD45BandEGR1areupregulatedinthepresenceofflavopiridol[2].PROTOCOLKinaseAssay[1]Briefly,lysatescontainingapproximately3×106cellsareincubatedwith50μMLEVD-AFC(caspase4substrate)orLETD-AFC(caspase8substrate)containing10mMdithiothretiol(DTT).Caspase4activityismeasuredonehourafteradditionofsubstrateandcaspase8activityismeasured30minutesafteradditionofsubstrate.ReleaseoffreeAFCismeasuredwithaBeckman-CoulterDTX880multimodedetector.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Thecellstreatedwithflavopiridolarewashedafter4hourswithPBSandresuspendedinregulargrowthmedium(RPMI1640)supplementedwith10%humanserumandantibioticsfortheremainderoftheincubationtime.Inthecaseofflavopiridol/chloroquinesamples,chloroquineisre-addedinthefreshmediaafterflavopiridoliswashedat4hours.Foralltheotherconditions,cellsareincubatedwiththerespectivedrugsfor24hourscontinuously.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Cell.2021Apr15;184(8):2167-2182.e22.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CancerDiscov.2021Oct6;candisc.1848.2020.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•Biomaterials.2014Aug;35(24):6585-94.•Biomaterials.2014Aug;35(24):6585-94.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MahoneyE,etal.ERstressandautophagy:newdiscoveriesinthemechanismofactionanddrugresistanceofthecyclin-dependentkinaseinhibitorflavopiridol.Blood.2012Aug9;120(6):1262-1273.[2].KeskinH,etal.Complexeffectsofflavopiridolontheexpressionofprimaryresponsegenes.CellDiv.2012Mar29;7:11.[3].KimKS,etal.Thio-andoxoflavopiridols,cyclin-dependentkinase1-selectiveinhibitors:synthesisandbiologicaleffects.JMedChem.2000Nov2;43(22):4126-34.