MLN0905-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMLN0905Cat.No.:HY-15155CASNo.:1228960-69-7分?式:C??H??F?N?S分?量:486.56作?靶點(diǎn):Polo-likeKinase(PLK)作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥30mg/mL(61.66mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0552mL10.2762mL20.5525mL5mM0.4110mL2.0552mL4.1105mL10mM0.2055mL1.0276mL2.0552mL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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(shí)驗(yàn)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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.14mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.14mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性MLN0905?種有效的Polo樣激酶1(PLK1)抑制劑，具有?服活性。MLN0905對PLK1具有抑制效?，IC50值為2nM。MLN0905可?于癌癥研究。IC50&TargetPLK12nM(IC50)體外研究MLN0905(compound12c)hasinhibitorypotencyagainstPLK1withanIC50valueof2nM[1].MLN0905exhibitspotentactivitiesforCdc25CwithanEC50valueof33nM[1].MLN0905showsinhibitoryeffectsonHT29,HCT116,H460,andA375celllineswithLD50valuesof22nM,56nM,89nMand34nM,respectively[1].MLN0905(125nM)showsstrongmitoticarrestandmonopolarspindleformationinHT-29cells[1].MLN0905suppressesthegrowthoflymphomacelllineswithIC50valuesrangingfrom3-24nM[2].體內(nèi)研究MLN0905(p.o.;50mg/kg)showsahighsustainedPDresponseinnudemiceHT29xenografttumors[1].MLN0905(p.o.;6.25,12.5,25,50mg/kg)exhibitssignificantantitumoractivitiesinmiceHT29xenografttumors[1].MLN0905(p.o.;0-14.5mg/kg;daily,QD×3/week)hasmarkedantitumoreffectsinkindsoflymphomaxenograftmodel[1][2].AnimalModel:Tumor(HT29)xenograftmodel[1]Dosage:0-50mg/kgAdministration:P.O;daily,QD×3/weekResult:Observedantitumoractivity,tumorstasisorregressionandwell-toleratedoraldoses.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Theranostics.2022;12(8):3911-3927.?PLoSNeglTropDis.2016Jan11;10(1):e0004356.?DepartmentofPathology.UniversityofCalifornia.2016.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].DuffeyMO,etal.Discoveryofapotentandorallybioavailablebenzolactam-derivedinhibitorofPolo-likekinase1(MLN0905).JMedChem.2012Jan12;55(1):197-208.[2].ShiJQ,etal.MLN0905,asmall-moleculeplk1inhibitor,inducesantitumorresponsesinhumanmodelsofdiffuselargeB-celllymphoma.MolCancerTher.2012Sep;11(9):2045-53.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf