NU6140-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENU6140Cat.No.:HY-107419CASNo.:444723-13-1分⼦式:C₂₃H₃₀N₆O₂分⼦量:422.52作⽤靶点:CDK;AuroraKinase作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(591.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3668mL11.8338mL23.6675mL5mM0.4734mL2.3668mL4.7335mL10mM0.2367mL1.1834mL2.3668mL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。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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.92mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NU6140⼀种选择性的CDK2-cyclinA抑制剂(IC50，0.41μM)，对其选择性对其他CDK的10-36倍[1]。NU6140有效抑制AuroraA和AuroraB的活性，IC50值分别为67和35nM[2]。增强诱导凋亡的作⽤，抗肿瘤作⽤[1][2]。IC50&Targetcdk2-cyclinACDK1-CyclinBCDK4-CyclinDcdk5-p250.41μM(IC50)6.6μM(IC50)5.5μM(IC50)15μM(IC50)cdk7-cyclinHAuroraAAuroraB3.9μM(IC50)67nM(IC50)35nM(IC50)体外研究NU6140islessactiveonCDK1-cyclinB,CDK4-cyclinD,CDK5-p25andCDK7-cyclinH,withIC50sof6.6,5.5,15and3.9μM,respectively[1].NU6140increasescatalyticactivityofcapase-9andcapase-3,causesincreaseinthesub-G1apoptoticcellpopulation[1].户使⽤本产品发表的科研⽂献•bioRxiv.2019Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PennatiM,etal.Potentiationofapoptosisbythenovelcyclin-dependentkinaseinhibitorNU6140:apossibleroleforsurvivindown-regulation.MolCancerTher.2005Sep;4(9):1328-37.[2].JordaR,etal.HowSelectiveArePharmacologicalInhibitorsofCell-Cycle-RegulatingCyclin-DependentKinases?MedChem.2018Oct25;61(20):9105-9120.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl