Palbociclib-isethionate-PD-0332991-isethionate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPalbociclibisethionateCat.No.:HY-A0065CASNo.:827022-33-3Synonyms:PD0332991isethionate分⼦式:C₂₆H₃₅N₇O₆S分⼦量:573.66作⽤靶点:CDK作⽤通路:CellCycle/DNADamage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H2O:50mg/mL(87.16mM;Needultrasonic)DMSO:10mg/mL(17.43mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7432mL8.7160mL17.4319mL5mM0.3486mL1.7432mL3.4864mL10mM0.1743mL0.8716mL1.7432mL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、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>>90%(20%SBE-β-CDinsaline)1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1mg/mL(1.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Palbociclib(PD0332991)isethionate⼀种具有⼝服活性的CDK4和CDK6选择性抑制剂，IC50值分别为11nM和16nM。Palbociclibdihydrochloride对癌细胞具有抗增殖活性，并诱导其细胞周期阻滞，可⽤于HR阳性和HER2性乳腺癌，以及肝细胞癌的相关研究[1][3][4]。IC50&TargetCdk4/cyclinD3Cdk4/cyclinD1Cdk6/cyclinD2DYRK1A9nM(IC50)11nM(IC50)16nM(IC50)2000nM(IC50)MAPK8000nM(IC50)体外研究Palbociclibdihydrochloride(0-1μM,24h)inhibitsRbPhosphorylationatSer795inMDA-MB-435cellswithanIC50valueof0.063μM,andobtainssimilareffectsonbothSer780andSer795phosphorylationintheColo-205coloncarcinoma[1].Palbociclibdihydrochloride(0-10μM,24h)arrestsMDA-MB-453cellsexclusivelyinG1phase[1].Palbociclibdihydrochloride(500nM,7days)increasesexpressionofhomologousgenes(H2d1,H2k1,andB2m)inMDA-MB-453andMDA-MB-361cells[2].Palbociclibdihydrochloride(0-1μM,6days)inhibitsgrowthofseveralluminalER-positiveaswellasHER2-amplifiedbreastcancercelllines,withIC50valuesrangingfrom4nMto1μM[3].Palbociclibdihydrochloride(0-1μM,3days)inhibitstheproliferationofhumanlivercancercelllineswithIC50valuesrangingfrom0.01μMto3.49μM,andinducesareversiblecellcyclearrest[4].CellCycleAnalysis[1]CellLine:MDA-MB-453cellsConcentration:0-1μMIncubationTime:24hResult:ArrestedMDA-MB-453cellsinG1.CellProliferationAssay[3]CellLine:ER-positiveaswellasHER2-amplifiedbreastcancercelllines(MDA-MB-175,ZR-75-30,CAMA-1,etc.)Concentration:0-10μMIncubationTime:6daysResult:InhibitedgrowthofluminalER-positiveaswellasHER2-amplifiedbreastcancercelllines.2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Palbociclibisethionate(oraladminstration,75or150mg/kg,dailyfor14days)producesrapidtumorregressionsanddelaystumorgrowth[1].Palbociclibisethionate(oraladminstration,90mg/kg,dailyfor12days)reducesTregnumbersandtheTreg:CD8ratiointhespleenandlymphnodesintumor-freemice,demonstratingthetumor-independenteffects[2].Palbociclibisethionate(oraladministration,100mg/kg,dailyfor1week)haspotentantitumoureffectsingeneticallyengineeredmosaicmousemodeloflivercancer[4].AnimalModel:MicebearingColo-205coloncarcinomaxenografts(p16deleted)[1]Dosage:75,150mg/kg,dailyfor14daysAdministration:OraladminstrationResult:Producedrapidtumorregressionsandacorrespondingtumorgrowthdelayof~50days.AnimalModel:Tumor-freefemaleFVBmice[2]Dosage:90mg/kg(dilutedin50nMsodiumD-lactate),dailyfor12daysAdministration:OraladminstrationResult:ReducedtotalthymicmassandimmatureCD4+andCD8+double-positivethymocytes,andincreasedthefractionsofCD4+andCD8+single-positivethymocytes.AnimalModel:Geneticallyengineeredmosaicmousemodeloflivercancer(Myc;p53-sgRNA)[4]Dosage:100mg/kg,dailyfor1week.Administration:OraladminstrationResult:Decreasedtheluminescencesignalinliveranddelayedtumourgrowth.户使⽤本产品发表的科研⽂献•Nature.2020Dec;588(7836):169-173.•Nature.2020Jul;583(7817):620-624.•Nature.2017Aug24;548(7668):471-475.•Nature.2017Jun15;546(7658):426-430.•NatMethods.2022Mar;19(3):331-340.Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].FryDW,etal.Specificinhibitionofcyclin-dependentkinase4/6byPD0332991andassociatedantitumoractivityinhumantumorxenografts.MolCancerTher.2004Nov;3(11):1427-38.[2].GoelS,etal.CDK4/6inhibitiontriggersanti-tumourimmunity.Nature.2017Aug24;548(7668):471-475.[3].RichardSFinn,etal.PD0332991,aselectivecyclinDkinase4/6inhibitor,preferentiallyinhibitsproliferationofluminalestrogenreceptor-positivehumanbreastcancercelllinesinvitro.BreastCancerRes.2009;11(5):R77.[4].BollardJ,etal.Palbociclib(PD-0332991),aselectiveCDK4/6inhibitor,restrictstumourgrowthinpreclinicalmodelsofhepatoc