XMU-MP-3-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEXMU-MP-3Cat.No.:HY-136531CASNo.:2031152-08-4分?式:C??H??F?N?O分?量:536.55作?靶點:Btk;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(186.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8638mL9.3188mL18.6376mL5mM0.3728mL1.8638mL3.7275mL10mM0.1864mL0.9319mL1.8638mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.66mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.66mM);ClearsolutionBIOLOGICALACTIVITY?物活性XMU-MP-3?種有效的?共價BTK抑制劑，在10μMATP存在下，對BTKWT和BTKC481S突變型的IC50分別為10.7nM和17.0nM。XMU-MP-3也誘導凋亡(apoptosis)[1]。IC50&TargetIC50:10.7nM(BTKWT),17.0nM(BTKC481S),Apoptosis[1]體外研究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.體內(nèi)研究XMU-MP-3(25and50mg/kg)substantiallysuppressestumorgrowthinmousexenograftmodels[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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