CAN508-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECAN508Cat.No.:HY-100429CASNo.:140651-18-9分⼦式:C₉H₁₀N₆O分⼦量:218.22作⽤靶点:CDK作⽤通路:CellCycle/DNADamage储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:250mg/mL(1145.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.5825mL22.9127mL45.8253mL5mM0.9165mL4.5825mL9.1651mL10mM0.4583mL2.2913mL4.5825mL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(protectfromlight)。-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:≥2.08mg/mL(9.53mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性CAN508⼀种有效的、ATP竞争性抑制CDK9/cyclinT1，IC50为0.35μM。CAN508对CDK9/cyclinT1⽐对其他的CDK/cyclin⾼出38倍的选择性。CAN508具有抗肿瘤活性。IC50&TargetCDK9/cyclinT1CDK2/cyclinEcdk2/cyclinACdk4/cyclinD10.35μM(IC50)20μM(IC50)69μM(IC50)13.5μM(IC50)CDK7/cyclinHCdk1/cyclinB26μM(IC50)44μM(IC50)体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl