T025-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemET025Cat.No.:HY-112296CASNo.:2407433-00-3分⼦式:C₂₁H₁₈N₈分⼦量:382.42作⽤靶点:CDK;Apoptosis;DYRK作⽤通路:CellCycle/DNADamage;Apoptosis;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:8.25mg/mL(21.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6149mL13.0746mL26.1493mL5mM0.5230mL2.6149mL5.2299mL10mM0.2615mL1.3075mL2.6149mL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。-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。BIOLOGICALACTIVITY⽣物活性T025⼝服有效的Cdc2-like激酶(CLK)抑制剂，对CLK1，CLK2，CLK3，CLK4，DYRK1A，DYRK1B和DYRK2的Kd分别为4.8，0.096，6.5，0.61，0.074，1.5和32nM。T025诱导caspase-3/7介导的细胞凋亡(apoptosis)。T025可降低CLK依赖性磷酸化。T025在⾎液和实体癌细胞系中均具有抗增殖活性(IC50值：30-300nM)。T025具有抗肿瘤功效，主⽤于MYC驱动的疾病研究。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetCLK2CLK4CLK1CLK30.096nM(Kd)0.61nM(Kd)4.8nM(Kd)6.5nM(Kd)DYRK1ADYRK1BDYRK20.074nM(Kd)1.5nM(Kd)32nM(Kd)体外研究T025(0-1000nM;72hours)significantlysuppressesthegrowthofMDA-MB-468cellsinadose-dependentmanner[1].T025(0-1000nM;6hours)reducesphosphorylationlevelsinMDA-MB-468cells[1].CellViabilityAssay[1]CellLine:MDA-MB-468cellsConcentration:1,10,100and1000nMIncubationTime:72hoursResult:Resultedinconcentrationdependentgrowthinhibition.WesternBlotAnalysis[1]CellLine:MDA-MB-468cellsConcentration:0,10,30,100,300and1000nMIncubationTime:6hoursResult:DecreasedbothpCLK2andCLK2.体内研究T025(50mg/kg;p.o.;2,4,8hours,Balb/cnudemice(7to8week-oldfemales).)suppresstheCLK-dependentphosphorylationandinduceskippingexoninvariousgenes[1].T025(50mg/kg;p.o.;twicedailyon2daysperweek,for3weeks,Balb/cnudemice(7to8week-oldfemales).)inhibitsMDA-MB-468xenograftmicetumorgrowthandwithoutaffectbodyweight[1].AnimalModel:Balb/cnudemice(7to8week-oldfemales)[1]Dosage:50mg/kgAdministration:Oraladministration;2,4,8hours.Result:pCLK2detectedwithimmunohistochemistryandimmunoblottingdecreased,byareductionintheRPS6KB1exon7andBCLAF1exon11percentagesplice-in(PSI)values.AnimalModel:Balb/cnudemice(7to8week-oldfemales)[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:50mg/kgAdministration:Oraladministration;twicedailyon2daysperweek,for3weeks.Result:Suppressedtumorgrowthand<10%nadirbodyweightloss.REFERENCES[1].IwaiK,etal.Anti-tumorefficacyofanovelCLKinhibitorviatargetingRNAsplicingandMYC-dependentvulnerability.EMBOMolMed.2018Jun;10(6):e8289.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap