ON1231320-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEON1231320Cat.No.:HY-100789CASNo.:1312471-39-8分?式:C??H??F?N?O?S分?量:467.45作?靶點:Polo-likeKinase(PLK);Apoptosis作?通路:CellCycle/DNADamage;Apoptosis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(53.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1393mL10.6963mL21.3927mL5mM0.4279mL2.1393mL4.2785mL10mM0.2139mL1.0696mL2.1393mL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%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.35mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性O(shè)N1231320?種?度特異性的polo樣激酶2(PLK2)抑制劑，IC50為0.31μM。ON1231320在有絲分裂G2/M期阻斷腫瘤細(xì)胞周期進程，導(dǎo)致細(xì)胞凋亡。ON1231320?種芳磺酰吡啶并嘧啶酮，具有抗腫瘤活性。IC50&TargetPLK2PLK1PLK3PLK40.31μM(IC50)>10μM(IC50)>10μM(IC50)>10μM(IC50)體外研究ON1231320(Compound7ao)hasnoinhibitoryactivityagainstPLK1,PLK3andPLK4(allIC50>10μM)[1].ON1231320(0-5μM;24hours)activatesprogrammedcelldeathinhumantumorcells[1].ON1231320inhibitscellproliferationin16tumorcelllines(DU145,MCF-7,BT474,SK-OV-3,MIA-PaCa-2,SK-MEL-28,A549,U87,COLO-205,HELA,H1975,RAJI,U205,K562,GRANTA-519;IC50=0.035-0.2μM)[1].ON1231320doesnotappreciablyinhibittubulinpolymerization[1].ON1231320doesnotaffectnormalhumanfibroblasts[2].ApoptosisAnalysis[1]CellLine:U2OScellsConcentration:0-5μMIncubationTime:24hoursResult:IncreasedtheactivityofCaspases3/7inadose-dependentmanner.Inducedapoptosis.體內(nèi)研究ON1231320(Compound7ao;75mg/kg;IP;alternatedays(Q2D)for20days)resultsinsignificantinhibitionoftumorgrowth[1].AnimalModel:6-8weekoldNCRnu/nufemalemicewithMDAMB-231triplenegativebreastcancercells[1]Dosage:75mg/kgAdministration:IP;alternatedays(Q2D)for20daysResult:Resultedinsignificantinhibitionoftumorgrowth(86.5%)REFERENCES[1].MVRamanaReddy,etal.Discoveryof2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one(7ao)asapotentselectiveinhibitorofPololikekinase2(PLK2).BioorgMedChem.2016Feb15;24(4):521-44.[2].ShashidharS.Jatiani,etal.Abstract643:TargetingcancerwithaselectiveATP-mimeticinhibitorofpololikekinase-2.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap