Samuraciclib-hydrochloride-hydrate-CT7001-hydrochloride-hydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESamuraciclibhydrochloridehydrateCat.No.:HY-103712BSynonyms:CT7001hydrochloridehydrate;ICEC0942hydrochloridehydrate分⼦式:C₂₂H₃₀N₆O.(₂.₅HCl).(₂H₂O)分⼦量:521.7作⽤靶点:CDK;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:4°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(191.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9168mL9.5841mL19.1681mL5mM0.3834mL1.9168mL3.8336mL10mM0.1917mL0.9584mL1.9168mL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(storedundernitrogen,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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.79mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.79mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(4.79mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Samuraciclib(CT7001)hydrochloridehydrate⼀种有效的，具有选择性，ATP竞争性和⼝服活性的CDK7抑制剂，IC50为41nM。Samuraciclibhydrochloridehydrate对CDK7的选择性分别CDK1，CDK2(IC50为578nM)，CDK5和CDK9的45倍，15倍，230倍和30倍。Samuraciclibhydrochloridehydrate以GI50值为0.2-0.3µM来抑制乳腺癌细胞系的⽣长，具有有效的抗肿瘤作⽤[1][2]。IC50&TargetCDK7CDK2CDK1CDK441nM(IC50)578nM(IC50)1.8μM(IC50)49μM(IC50)CDK5CDK6CDK99.4μM(IC50)31μM(IC50)1.2μM(IC50)体外研究Samuraciclibhydrochloridehydrate(ICEC0942;0-10µM;24hours;HCT116cells)treatmentpromotescellapoptosis[1].Samuraciclibhydrochloridehydrate(ICEC0942;0-10µM;24hours;HCT116cells)treatmentinducescellcyclearrest[1].Samuraciclibhydrochloridehydrate(ICEC0942;0-10µM;0-24hours;HCT116cells)treatmentinhibitsthephosphorylationofPolIICTDinadoseandtimedependentmannerinHCT116coloncancercells.SamuraciclibtrihydrochloridealsoinhibitsphosphorylationofCDK1,CDK2andretinoblastoma[1].Samuraciclib(ICEC0942)hydrochloridehydrateinhibitsthegrowthofMCF7,T47D,MDA-MB-231,HS578T,MDA-MB-468,MCF10AandHMECcellswithGI50valuesof0.18µM,0.32µM,0.33µM,0.21µM,0.22µM,0.67µMand1.25µM,respectively[1].ApoptosisAnalysis[1]CellLine:HCT116cellsConcentration:0µM,0.1µM,1µMand10µMIncubationTime:24hoursResult:Inducedcaspase3/7anddemonstratedPARPcleavage.CellCycleAnalysis[1]CellLine:HCT116cellsConcentration:0µM,0.01µM,0.1µM,1µMand10µMIncubationTime:24hours2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ShowedaccumulationofcellsinG2/M.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0µM,0.01µM,0.1µM,1µMand10µMIncubationTime:0hour,4hours,8hours,16hoursor24hoursResult:PolIICTDphosphorylationwasinhibitedinadoseandtimedependentmannerinHCT116coloncancercells.体内研究Samuraciclib(ICEC0942;100mg/kg;oralgavage;daily;for14days;femalenu/nu-BALB/cathymicnudemice)hydrochloridehydratetreatmentinhibitstumorgrowthby60%atday14,andisaccompaniedbyhighlysignificantreductionsinPolIISer2andSer5phosphorylationinPBMCsandintumors[1].ThecombinationofSamuraciclib(ICEC0942)hydrochloridehydrateandICI47699treatmentshowscompletegrowtharrestofestrogenreceptor(ER)-positivetumorxenografts[1].AnimalModel:Femalenu/nu-BALB/cathymicnudemice(7-weekold)withMCF7cells[1]Dosage:100mg/kgAdministration:Oralgavage;daily;for14daysResult:Atday14,tumorgrowthwasinhibitedby60%.户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2019Jun25;116(26):12986-12995.•CellDeathDis.2019Aug9;10(8):602.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PatelH,etal.ICEC0942,anOrallyBioavailableSelectiveInhibitorofCDK7forCancerTreatment.MolCancerTher.2018Jun;17(6):1156-1166.[2].HazelP,etal.InhibitorSelectivityforCyclin-DependentKinase7:AStructural,Thermodynamic,andModellingStudy.ChemMedChem.2017Mar7;12