XMD16-5-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEXMD16-5Cat.No.:HY-101243CASNo.:1345098-78-3分?式:C??H??N?O?分?量:416.48作?靶點:Tyrosinase作?通路:MetabolicEnzyme/Protease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(240.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4011mL12.0054mL24.0108mL5mM0.4802mL2.4011mL4.8022mL10mM0.2401mL1.2005mL2.4011mL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(dāng)?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(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(6.00mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性XMD16-5?種有效的TNK2抑制劑，對于D163E和R806Q突變體的IC50值分別為16和77nM。IC50&TargetIC50:16nM(TNK2,D163Emutation),77nM(TNK2,R806Qmutation)[1]體外研究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