Samuraciclib-hydrochloride-hydrate-CT7001-hydrochloride-hydrate-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESamuraciclibhydrochloridehydrateCat.No.:HY-103712BSynonyms:CT7001hydrochloridehydrate;ICEC0942hydrochloridehydrate分?式:C??H??N?O.(?.?HCl).(?H?O)分?量:521.7作?靶點:CDK;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:4°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(191.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9168mL9.5841mL19.1681mL5mM0.3834mL1.9168mL3.8336mL10mM0.1917mL0.9584mL1.9168mL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備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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、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:≥2.5mg/mL(4.79mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:2.5mg/mL(4.79mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Samuraciclib(CT7001)hydrochloridehydrate?種有效的，具有選擇性，ATP競爭性和?服活性的CDK7抑制劑，IC50為41nM。Samuraciclibhydrochloridehydrate對CDK7的選擇性分別CDK1，CDK2(IC50為578nM)，CDK5和CDK9的45倍，15倍，230倍和30倍。Samuraciclibhydrochloridehydrate以GI50值為0.2-0.3μM來抑制乳腺癌細胞系的?長，具有有效的抗腫瘤作?[1][2]。IC50&TargetCDK7CDK2CDK1CDK441nM(IC50)578nM(IC50)1.8μM(IC50)49μM(IC50)CDK5CDK6CDK99.4μM(IC50)31μM(IC50)1.2μM(IC50)體外研究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?邊的抑制劑?師www.MedChemEResult:ShowedaccumulationofcellsinG2/M.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0μM,0.01μM,0.1μM,1μMand10μMIncubationTime:0hour,4hours,8hours,16hoursor24hoursResult:PolIICTDphosphorylationwasinhibitedinadoseandtimedependentmannerinHCT116coloncancercells.體內(nèi)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%.戶使?本產(chǎn)品發(fā)表的科研?獻?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