SP-96-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESP-96Cat.No.:HY-131339CASNo.:2682114-54-9分⼦式:C₂₅H₂₀FN₇O分⼦量:453.47作⽤靶点: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:100mg/mL(220.52mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2052mL11.0261mL22.0522mL5mM0.4410mL2.2052mL4.4104mL10mM0.2205mL1.1026mL2.2052mL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%cornoilSolubility:≥2.5mg/mL(5.51mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性SP-96⼀种⾼效、选择性和ATP竞争性AuroraB抑制剂，IC50为0.316nM，对FLT3和KIT具有>2000倍选择性。SP-96在NCI60筛选中表现出选择性⽣长抑制，对MDA-MD-468等乳腺癌细胞具有选择性(GI50=107nM)。SP-96可⽤于三性乳腺癌(TNBC)的相关研究。IC50&TargetAuroraAAuroraB18.975nM(IC50)0.316nM(IC50)体外研究SP-96isahighlypotent,selectiveandnon-ATP-competitiveAuroraB(IC50=0.316nM)inhibitorandshows>2000foldselectivityagainstFLT3(IC50=1475.6nM)andKIT(IC50=1307.6nM)[1].SP-96(0-1µM;24hours)isnotpromiscuous,ratherselectiveforafewcelllines,itinhibitsMDA-MB-468,CCRF-CEM,COLO205andA498cellgrowthwithGI50valuesof107nM,47.4nM,50.3nMand53.2nM,respectively[1].SP-96(63.2nM)inhibitsAuroraBactivityinH460cellsbythecharacteristicsofincreasedDNAcontent,anditincreasescellvolumewithenormousnucleus[1].SP-96(0-2µM)inhibitsAuroraBenzymaticactivitywithanIC50of0.316nMandinhibitsAuroraAwithobservedIC50valueof18.975nM.SP-96shows>2000foldselectivityagainstFLT3(IC50=1475.6nM)andKIT(IC50=1307.6nM).Meanwhile,itexhibitsinhibitoryeffectsonotherreceptortyrosinekinases(RTKs)namelyEGFR,RETandHER2withIC50value≥2µM[1].CellViabilityAssay[1]CellLine:MDA-MB-468,CCRF-CEM,COLO205andA498cellConcentration:0-1µMIncubationTime:24hoursResult:ShowedgoodinhibitoryactivityonMDA-MB-468cells.REFERENCES[1].NagaRajivLakkaniga,etal.DiscoveryofSP-96,thefirstnon-ATP-competitiveAuroraKinaseBinhibitor,forreducedmyelosuppression.EurJMedChem.2020Jul12;203:112589.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F