AZ6102-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZ6102Cat.No.:HY-12975CASNo.:1645286-75-4分?式:C??H??N?O分?量:428.53作?靶點:PARP作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(58.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3336mL11.6678mL23.3356mL5mM0.4667mL2.3336mL4.6671mL10mM0.2334mL1.1668mL2.3336mL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(5.83mM);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(5.83mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.83mM);ClearsolutionBIOLOGICALACTIVITY?物活性AZ6102?種有效的TNKS1和TNKS2雙重抑制劑，IC50值分別為3nM和1nM，選擇性對PARP家族其他蛋?的100多倍，對PARP1，PARP2和PARP6的IC50值分別為2.0μM，0.5μM和>3μM。IC50&TargetTNKS2TNKS1PARP1PARP22nM(IC50)3nM(IC50)2μM(IC50)0.5μM(IC50)體外研究AZ6102isapotentdualTNKS1andTNKS2inhibitor,withIC50sof3nMand1nM,respectively.AZ6102alaohas100-foldselectivityagainstotherPARPfamilyenzymes,withIC50sof2.0μM,0.5μM,and>3μM,forPARP1,PARP2,andPARP6,respectively.AZ6102showsWntpathwayinhibitioninDLD-1cells[1].PROTOCOLKinaseAssay[1]Theassayisconductedusing0.11μMoftankyrase-1proteinand3μMnicotinamideadeninedinucleotide(NAD+,2.12μM3H-NAD+withaspecificradioactivityof1690Ci/mol,0.88μMbiotin-NAD+),inpH7.5Trisbuffer(60mMTris,1mMDTT,0.01%(v/v)Tween-20?,2.5mMMgCl2,0.3mg/mLBSA).ForIC50determination,10mMDMSOstocksolutionofacompound(AZ6102)issequentiallydilutedbytwo-foldinDMSO,andaliquotsofthedilutedsolutionsaretransferredto384-wellassayplatesandmixedwithTankyrase-1solution[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?JMolMed(Berl).2019Aug;97(8):1183-1193.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JohannesJW,etal.Pyrimidinonenicotinamidemimeticsasselectivetankyraseandwntpathwayinhibitorssuitableforinvivopharmacology.ACSMedChemLett.2015Jan13;6(3):254-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica