Dalpiciclib-hydrochloride-SHR-6390-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDalpiciclibhydrochlorideCat.No.:HY-114338ASynonyms:SHR-6390hydrochloride分?式:C??H??ClN?O?分?量:483.01作?靶點(diǎn):CDK作?通路:CellCycle/DNADamage儲存?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:5mg/mL(10.35mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0704mL10.3518mL20.7035mL5mM0.4141mL2.0704mL4.1407mL10mM0.2070mL1.0352mL2.0704mL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(fù)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(sealedstorage,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?。BIOLOGICALACTIVITY?物活性Dalpiciclib(SHR-6390)hydrochloride?種具有?服活性和?選擇性的CDK4/6抑制劑，IC50值分別為12.4nM和9.9nM。Dalpiciclibhydrochloride對乳腺癌和?道鱗狀細(xì)胞癌顯?出抗腫瘤活性。IC50&TargetCDK4CDK612.4nM(IC50)9.9nM(IC50)體外研究Dalpiciclibhydrochloride(0-4μM,72h)inhibitscellproliferationinadose-dependentmanner[3].1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDalpiciclibhydrochloride(0-10μM,6d)inhibitstheproliferationofretinoblastoma-positivetumorcelllines[4].CellProliferationAssay[3]CellLine:Eca109,Eca9706andKYSE-510ESCCcelllinesConcentration:0-4μMIncubationTime:72?hoursResult:Inhibitedcellproliferationinadose-dependentmanner,withEca109beingtherelativesensitiveoneandEca9706beingtherelativeresistantone.CellViabilityAssay[4]CellLine:MCF7,MCF7/TR,BT-474/TcelllinesConcentration:0-10μMIncubationTime:6?daysResult:InhibitedMCF7/TRcells,parentalMCF7cellsandBT-474/TresistantcellswiththeIC50valuesof229.5,115.4and210.7nM,respectively.體內(nèi)研究Dalpiciclibhydrochloride(oralgavage;150mg/kg;onceweekly;3weeks)showsantitumoractivityagainstESCCxenografts[3].DalpiciclibhydrochloridecombinedwithPaclitaxel(PTX)orCisplatin(CDDP)offersynergisticinhibitoryeffectsinESCCxenografts[3].Dalpiciclibhydrochloride(oralgavage;37.5mg/kg,75mg/kg,150mg/kg;oncedaily;30days)showsantitumoractivityinhumanxenograftmodels[4].AnimalModel:NOD/SCIDmice(ESCCPDXsmodels)[3]Dosage:150mg/kgAdministration:Oralgavage;150mg/kg;onceweekly;3weeksResult:Suppressedthegrowthoftumor.AnimalModel:5-week-oldfemaleBalb/cA-nudemicesubcutaneouslyinoculatedMCF7/ARO,COLO205andU87MG[4]Dosage:37.5mg/kg,75mg/kg,150mg/kgAdministration:Oralgavage;37.5mg/kg,75mg/kg,150mg/kg;oncedaily;30daysResult:Causedregressionofalltumorxenograftsatthehighestdosetested.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].JoseManuelPerez-Garcia,etal.Perez-GarciaJM,CortesJ,Llombart-CussacA.CDK4/6inhibitorsinbreastcancer:spottingthedifference.NatMed.2021Nov;27(11):1868-1869.[2].PinZhang,etal.Aphase1studyofdalpiciclib,acyclin-dependentkinase4/6inhibitorinChinesepatientswithadvancedbreastcancer.BiomarkRes.2021Apr12;9(1):24.[3].JiayuanWang,etal.CDK4/6inhibitor-SHR6390exertspotentantitumoractivityinesophagealsquamouscellcarcinomabyinhibitingphosphorylatedRbandinducingG1cellcyclearrest.JTranslMed.2017Jun2;15(1):127.[4].FeiLong,etal.PreclinicalcharacterizationofSHR6390,anovelCDK4/6inhibitor,invitroandinhumantumorxenograftmodels.CancerSci.2019Apr;110(4):1420-1430.McePdfHeightCaution:Producthasnot