BAY-293-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY-293Cat.No.:HY-114398CASNo.:2244904-70-7分⼦式:C₂₅H₂₈N₄O₂S分⼦量:448.58作⽤靶点:Ras作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥125mg/mL(278.66mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2293mL11.1463mL22.2926mL5mM0.4459mL2.2293mL4.4585mL10mM0.2229mL1.1146mL2.2293mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.64mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.64mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BAY-293⼀种有价值的化学探针，通过破坏KRAS-SOS1相互作⽤从⽽阻断RAS活化，IC50为21nM。BAY-293⼀种有效的SOS1抑制剂。SOS1⼀种鸟苷酸交换因⼦(GEF)，也RAS的激活剂[1]。IC50&TargetKRAS-SOS121nM(IC50)体外研究BAY-293inhibitstheactivationofRASinHeLacells,withIC50valuesinthesubmicromolarrange[1].BAY-293(595nM-3580nM;72hours)showsefficientantiproliferativeactivityagainstwild-typeKRAScelllines(K-562,MOLM-13)andcelllineswithKRASG12Cmutation(NCI-H358,Calu-1)[1].BAY-293efficientlyinhibitspERKlevelsinK-562cellsafterincubationfor60minwithoutaffectingtotalproteinlevelsofERK[1].CellProliferationAssay[1]CellLine:K-562,MOLM-13,H358andCalu-1celllinesConcentration:595-3580nMIncubationTime:72hoursResult:IC50sof1,090±170nM,995±400nM,3,480±100nMand3,190±50nMforK-562,MOLM-13,H358andCalu-1cells,respectively.户使⽤本产品发表的科研⽂献•SignalTransductTargetTher.2022Sep12;7(1):317.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HilligRC,etal.DiscoveryofpotentSOS1inhibitorsthatblockRASactivationviadisruptionoftheRAS-SOS1interaction.ProcNatlAcadSciUSA.2019Feb12;116(7):2551-2560.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu