NSC-70220-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENSC-70220Cat.No.:HY-101796CASNo.:4551-00-2分⼦式:C₂₂H₁₅NO₂分⼦量:325.36作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:12.5mg/mL(38.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0735mL15.3676mL30.7352mL5mM0.6147mL3.0735mL6.1470mL10mM0.3074mL1.5368mL3.0735mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.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:≥1.25mg/mL(3.84mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(3.84mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性NSC-70220⼀种选择性的变构SOS1抑制剂。NSC-70220抑制变构位点激活，并部分抑制催化位点激活。NSC-70220具有抗癌作⽤。IC50&TargetSOS1[1].体外研究Thegrowthinhibitoryrate(IR)=(averageODvalueinthecontrolgroup-averageODvalueinthetreatmentgroup)/averageODvalueinthecontrolgroup×100%arecompared.TreatmentswithNSC-70220at40μMandNSC-658497at30μMresultingrowthinhibitoryrateof29%and8%respectively.Thecombinationtreatmentresultsingrowthinhibitoryrateof54%,showingthesynergisticeffectofNSC-70220andNSC-658497oncellgrowthinhibition.ItisshowedthatthetreatmentwithNSC-658497at40μMfor2hoursaloneorincombìnationwiththetreatmentwith40μMofNSC-70220overnightresultedinlowerexpressionlevelsofP-AKTandP-ERK.Thetreatmentwlth40μMofNSC-70220overnightresultedinlowerexpressionlevelsofP-ERK[1].PROTOCOLCellAssay[1]MIApaca-2cells(KRASG12C)aresubjectedtoa3-dayproliferationassayfollowingtreatmentwithSOS1-IN-1(NSC-70220:40μM),treatmentwithNSC-658497(30μM)andtreatmentwithacombinationofSOS1-IN-1(40μM)andNSC-658497(30μM).DMSOisusedasthenegativecontrol[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].ARYLSULFONOHYDRAZIDES.WO2016077793A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu