Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECAN508Cat.No.:HY-100429CASNo.:140651-18-9分?式:C?H??N?O分?量:218.22作?靶點:CDK作?通路:CellCycle/DNADamage儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數據體外實驗DMSO:250mg/mL(1145.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.5825mL22.9127mL45.8253mL5mM0.9165mL4.5825mL9.1651mL10mM0.4583mL2.2913mL4.5825mL請根據產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品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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:≥2.08mg/mL(9.53mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性CAN508?種有效的、ATP競爭性抑制CDK9/cyclinT1，IC50為0.35μM。CAN508對CDK9/cyclinT1?對其他的CDK/cyclin?出38倍的選擇性。CAN508具有抗腫瘤活性。IC50&TargetCDK9/cyclinT1CDK2/cyclinEcdk2/cyclinACdk4/cyclinD10.35μM(IC50)20μM(IC50)69μM(IC50)13.5μM(IC50)CDK7/cyclinHCdk1/cyclinB26μM(IC50)44μM(IC50)體外研究CAN508reducesthefrequencyofS-phasecellsofthecancercelllineHT-29inantiproliferationassays[1].CAN508(20-40μM;72hours)significantlyreducescellproliferationinadosedependentmannerinallthreeesophagealadenocarcinomacelllines(SKGT4,OE33andFLO-1cells)withIC50srangingfrom34.99to91.09μM[2].CAN508(40μM;72hours)increasesapoptosisinallthreeesophagealadenocarcinomacells[2].ApoptosisAnalysis[1]CellLine:SKGT4,OE33andFLO-1cellsConcentration:40μMIncubationTime:72hoursResult:Increasedapoptosisby2foldinallthreeesophagealadenocarcinomacellscomparedtountreatedcontrols.體內研究CAN508(60mg/kg;i.p.;dailyfor10days)hasantitumoreffectsinesophagealadenocarcinomaxenografts[1].AnimalModel:4weeks-oldfemalenudemice(esophagealadenocarcinomaxenografts)[1]Dosage:60mg/kgAdministration:I.p.;dailyfor10daysResult:Causedreductionoftumorgrowthstartingfrompost-treatmentdaythreewith50.83%reduction.REFERENCES[1].KrystofV,etal.4-arylazo-3,5-diamino-1H-pyrazoleCDKinhibitors:SARstudy,crystalstructureincomplexwithCDK2,selectivity,andcellulareffects.JMedChem.2006;49(22):6500-6509.[2].TongZ,etal.Antitumoreffectsofcyclindependentkinase9inhibitioninesophagealadenocarcinoma.Oncotarget.2017;8(17):28696-28710.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl