CCT251455-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECCT251455Cat.No.:HY-12603CASNo.:1400284-80-1分⼦式:C₂₆H₂₆ClN₇O₂分⼦量:503.98作⽤靶点:Mps1作⽤通路:CellCycle/DNADamage;Cytoskeleton储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(198.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9842mL9.9210mL19.8421mL5mM0.3968mL1.9842mL3.9684mL10mM0.1984mL0.9921mL1.9842mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.96mM);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%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.96mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.96mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CCT251455有效和选择性的有丝分裂激酶单极纺锤体1(MPS1)抑制剂，IC50值为3nM。IC50&TargetIC50:3nM(MPS1)[1]体外研究CCT251455isahighlypotentinhibitorofMPS1thatdemonstrateshighselectivityversuskinasestestedinabroadkinomeprofilingpanel.CCT251455inhibitsP-MPS1withanIC50of0.04μMincell-basedassayandhasaGI50of0.16μM[1].体内研究CCT251455demonstratesagoodoralpharmacokineticprofileinmouseandrataswellasinhibitionofMPS1activityinvivofollowingoraladministration[1].PROTOCOLCellAssay[1]HCT116cellsaretreatedwith0-20μMCCT251455for72h.CellviabilityismeasuredusingtheMTTassay[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1][1]HumanHCT116coloncarcinomacellsarescinjectedbilaterallyintheflanksoffemaleCrTac:NCr-Fox1(nu)athymicmice.Oncetumorsreachameandiameterof8mm(day15),micearedosedtwiceata12hintervalswith50,75,or100mg/kgofCCT251455in10%(v/v)DMSOand5%(v/v)Tween20insaline.Miceareculled(n=3pergroup)at2,10,and72haftertheseconddose.Tumorsaresnap-frozenandstoredat-80°Cuntilanalysis[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].NaudS,etal.Structure-baseddesignoforallybioavailable1H-pyrrolo[3,2-c]pyridineinhibitorsofmitotickinasemonopolarspindle1(MPS1).JMedChem.2013Dec27;56(24):10045-65.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappli