Flavopiridol-Hydrochloride-Alvocidib-Hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFlavopiridolHydrochlorideCat.No.:HY-10006CASNo.:131740-09-5Synonyms:AlvocidibHydrochloride;L86-8275Hydrochloride;HMR-1275Hydrochloride分?式:C??H??Cl?NO?分?量:438.3作?靶點(diǎn):CDK;Autophagy;HIV作?通路:CellCycle/DNADamage;Autophagy;Anti-infection儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥20mg/mL(45.63mM)H2O:≥20mg/mL(45.63mM)DMF:7.69mg/mL(17.55mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2815mL11.4077mL22.8154mL5mM0.4563mL2.2815mL4.5631mL10mM0.2282mL1.1408mL2.2815mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.67mg/mL(1.53mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.67mg/mL(1.53mM);ClearsolutionBIOLOGICALACTIVITY?物活性FlavopiridolHydrochloride(AlvocidibHydrochloride)?種CDK的?譜抑制劑，與ATP競爭性地抑制CDK1，CDK2和CDK4的活性，IC50值分別為30,170,100nM。IC50&TargetCDK1/CycB1CDK2/CycECDK4/CycD1MAP30nM(IC50)170nM(IC50)100nM(IC50)19000nM(IC50)PKCEGFR14000nM(IC50)22000nM(IC50)體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Cell.2021Apr15;184(8):2167-2182.e22.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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.