NU6140-DataSheet-生命科學(xué)試劑-MedChemExpressVIP

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENU6140Cat.No.:HY-107419CASNo.:444723-13-1分?式:C??H??N?O?分?量:422.52作?靶點:CDK;AuroraKinase作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(591.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3668mL11.8338mL23.6675mL5mM0.4734mL2.3668mL4.7335mL10mM0.2367mL1.1834mL2.3668mL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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.92mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.92mM);ClearsolutionBIOLOGICALACTIVITY?物活性NU6140?種選擇性的CDK2-cyclinA抑制劑(IC50，0.41μM)，對其選擇性對其他CDK的10-36倍[1]。NU6140有效抑制AuroraA和AuroraB的活性，IC50值分別為67和35nM[2]。增強誘導(dǎo)凋亡的作?，抗腫瘤作?[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)體外研究NU6140islessactiveonCDK1-cyclinB,CDK4-cyclinD,CDK5-p25andCDK7-cyclinH,withIC50sof6.6,5.5,15and3.9μM,respectively[1].NU6140increasescatalyticactivityofcapase-9andcapase-3,causesincreaseinthesub-G1apoptoticcellpopulation[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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