XMU-MP-3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXMU-MP-3Cat.No.:HY-136531CASNo.:2031152-08-4分⼦式:C₂₇H₂₇F₃N₈O分⼦量:536.55作⽤靶点:Btk;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(186.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8638mL9.3188mL18.6376mL5mM0.3728mL1.8638mL3.7275mL10mM0.1864mL0.9319mL1.8638mL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(4.66mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.66mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性XMU-MP-3⼀种有效的⾮共价BTK抑制剂，在10μMATP存在下，对BTKWT和BTKC481S突变型的IC50分别为10.7nM和17.0nM。XMU-MP-3也诱导凋亡(apoptosis)[1]。IC50&TargetIC50:10.7nM(BTKWT),17.0nM(BTKC481S),Apoptosis[1]体外研究XMU-MP-3(0.001-10000nM;48hours)inhibitsBTK-transformedBa/F3cellproliferationwithanIC50of11.4nM[1].XMU-MP-3(1-10000nM)inhibitstheproliferationofJeKo-1,RamosandNALM-6withIC50valuesof326.6nM,685.6nMand1065nM,respectively[1].XMU-MP-3(0.001-10000nM)maintainsinhibitorypotencywithanIC50of182.3nMagainstBTK(C481S)-Ba/F3cells[1].XMU-MP-3(5000nM)inducesapoptosisinBTK(C481S)Ba/F3cells[1].XMU-MP-3(10-1000nM;4hours)inhibitsboththeauto-andtrans-phosphorylationofBTKatthesiteofY223andY551inadose-dependentmannerinBTK-transformedBa/F3cells[1].CellProliferationAssay[1]CellLine:BTK-transformedandparentalBa/F3cellsConcentration:0.001,0.01,0.1,1,10,100,1000,10000nMIncubationTime:48hoursResult:InhibitedBTK-transformedBa/F3cellproliferationwithanIC50of11.4nM,whileitshowednegligibleanti-proliferativeeffectsonparentalwild-typeBa/F3cells(IC50>10000nM).WesternBlotAnalysis[1]CellLine:BTK-transformedBa/F3cellsConcentration:10,50,100,500,1000nMIncubationTime:4hoursResult:ThephosphorylationlevelsofBTKY223andY551werereducedsignificantlyatconcentrationsaslowas100nM,andcompletelysuppressedattheconcentrationof1000nM.体内研究XMU-MP-3(25and50mg/kg)substantiallysuppressestumorgrowthinmousexenograftmodels[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Nu/nuBALB/cmice(4-6weeksofage)bearingBTK-transformedBa/F3andRamosxenograftmodels[1]Dosage:25and50mg/kgAdministration:Treatedbytailveininjection;theinjectionvolumewas0.1mLper10g;dailyfor14daysResult:Significantlyreducedthetumorsizewithoutaffectinganimalweights.REFERENCES[1].FuGui,etal.ANon-CovalentInhibitorXMU-MP-3OverridesIbrutinib-ResistantBtkC481SMutationinB-cellMalignancies.BrJPharmacol.2019Dec;176(23):4491-4509.McePdfHeightCaution:Producthasnotbeenfullyv