LTURM34-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELTURM34Cat.No.:HY-101667CASNo.:1879887-96-3分?式:C??H??N?O?S分?量:414.48作?靶點:DNA-PK作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:65mg/mL(156.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4127mL12.0633mL24.1266mL5mM0.4825mL2.4127mL4.8253mL10mM0.2413mL1.2063mL2.4127mL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>>90%cornoilSolubility:≥3.25mg/mL(7.84mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性LTURM34?種特異的DNA-PK抑制劑(IC50=34nM)。與PI3K相?，LTURM34對DNA-PK的選擇性?170倍。LTURM34在多種腫瘤細(xì)胞系中顯?出有效的抗增殖活性[1]。IC50&TargetDNA-PKPI3KβPI4Kδ34nM(IC50)5.8μM(IC50)8.5μM(IC50)體外研究LTURM34showspotentinhibitionofDNA-PKwithexcellentselectivityovertheClassIPI3Kisoforms.TheIC50sare5.8and8.5μMforPI3Kβandδ,respectively.LTURM34ismoreconsistentlyactiveagainsttheselectedcelllines(11of16),butatbestshows54%inhibitionagainsttheHOP-92non-smallcelllungcancerline[1].PROTOCOLKinaseAssay[1]LTURM34isdissolvedat10mMinDMSOandstoredat-20°Cuntiluse.PI3Kenzymeactivityisdeterminedin50μLof20mMHEPESpH7.5,5mMMgCl2with180μMPIand10μMATP.Aftera60minincubationatroomtemperaturethereactionisstoppedbytheadditionof50μlofKinase-Glofollowedbyafurther15minincubation.Luminescenceisthenreadusingaluostarplatereader.LTURM34isdilutedin20%(v/v)DMSOatthendicatedconcentrationsinordertogenerateaconcentrationversusinhibitionofenzymeactivitycurvewhichisthenanalysedusingGraphPadPrismversion5.00forWindows,inordertocalculatetheIC50[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?GenomeRes.2021Mar;31(3):461-471.?CellRep.2020Jan14;30(2):497-509.e4.?Oncogenesis.2020Feb3;9(2):8.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MorrisonR,etal.Synthesis,structureelucidation,DNA-PKandPI3Kandanti-canceractivityof8-and6-aryl-substituted-1-3-benzoxazines.EurJMedChem.2016Mar3;110:326-39.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati