CB-6644-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECB-6644Cat.No.:HY-114429CASNo.:2316817-88-4分⼦式:C₂₉H₃₄ClFN₄O₅分⼦量:573.06作⽤靶点:Others作⽤通路:Others储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(174.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7450mL8.7251mL17.4502mL5mM0.3490mL1.7450mL3.4900mL10mM0.1745mL0.8725mL1.7450mL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(storedundernitrogen)。-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(3.63mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.63mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.63mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CB-6644⼀种选择性的RUVBL1/2复合体抑制剂。抑制RUVBL1/2的ATP酶活性，IC50为15nM[1]。具有抗癌活性[1]。体外研究CB-6644(20µM)interactswiththeRUVBL1/2complexinRamoscells[1].CB-6644(0.001-10μM;72hours)potentlykills123celllines(includingHCT116,NCI-1975,andHT29cells)withanEC50rangeof41to785nM[1].CellViabilityAssay[1]CellLine:123celllinessuchasHCT116,NCI-1975,andHT29cellsConcentration:0.001,0.01,0.1,1,and10μMIncubationTime:72hoursResult:PotentlykilledcellswithanEC50rangeof41to785nM.体内研究CB-6644(150mg/kg,oraladministration,10daysoftreatmentforSCID-beigemicebearingRamosxenograftmodels,30daysoftreatmentforSCID-beigemicebearingRPMI8226xenograftmodels)hasantitumoractivityinxenografttumormodelswithtumorgrowthinhibitions(TGIs)of68and81%,respectivelyinRamosxenograftmodelsandRPMI8226xenograftmodels[1].AnimalModel:SCID-beigemicebearinghumantumorxenograftsderivedfromeitherBurkitt’slymphoma(Ramos)ormultiplemyeloma(RPMI8226)celllines[1]Dosage:150mg/kgAdministration:Oralgavageonce(qd)ortwice(BID)daily,10daysoftreatmentforRamos,30daysoftreatmentforRPMI8226Result:Therewasnosignificantbodyweightlossinmice.TGIof68and81%inRamosandRPMI8226,respectively.户使⽤本产品发表的科研⽂献•CellRep.2022May24;39(8):110846.•FrontImmunol.04June2021.•Oncogene.2022May4.•bioRxiv.July11,2021.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].AssimonVA,etal.CB-6644IsaSelectiveInhibitoroftheRUVBL1/2ComplexwithAnticancerActivity.ACSChemBiol.2019Feb15;14(2):236-244.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme