XMD16-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXMD16-5Cat.No.:HY-101243CASNo.:1345098-78-3分⼦式:C₂₃H₂₄N₆O₂分⼦量:416.48作⽤靶点:Tyrosinase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(240.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4011mL12.0054mL24.0108mL5mM0.4802mL2.4011mL4.8022mL10mM0.2401mL1.2005mL2.4011mL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(6.00mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.00mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性XMD16-5⼀种有效的TNK2抑制剂，对于D163E和R806Q突变体的IC50值分别为16和77nM。IC50&TargetIC50:16nM(TNK2,D163Emutation),77nM(TNK2,R806Qmutation)[1]体外研究XMD16-5potentlyinhibitsthegrowthoftheTNK2mutantexpressingcelllineswhilehavinglittleornoeffectonthecontrolcellsouttothehighesttestedconcentrations(1,000nM).XMD16-5hasIC50sof16nMand77nMfortheD163EandR806Qmutations.TheeffectsofXMD16-5onTNK2celllinesarelargelyduetoon-targeteffectsonTNK2.Auto-phosphorylationofoverexpressedTNK2mutantscouldbeblockedwithTNK2inhibitorXMD16-5[1].PROTOCOLKinaseAssay[1]KinasetargetsaretestedwithbiochemicalenzymatickinaseassaysusingtheSelectScreenKinaseProfilingServicetodetermineIC50values.Thecompounds(XMD16-5)areassayedat10concentrations(3-foldserialdilutionsstartingfrom1μM)atanATPconcentrationequaltotheATPKm[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Cellsaretreatedwiththefollowinginhibitorsfor72hours:dasatinib,AIM-100,XMD8-87andXMD16-5.Cellviabilityismeasuredusingamethanethiosulfonate(MTS)-basedassayandabsorbance(490nm)isreadat1and3hoursafteraddingreagent[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].MaxsonJE,etal.IdentificationandCharacterizationofTyrosineKinaseNonreceptor2MutationsinLeukemiathroughIntegrationofKinaseInhibitorScreeningandGenomicAnalysis.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat