S516-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemES516Cat.No.:HY-130233CASNo.:1016543-77-3分?式:C??H??N?O?S分?量:437.47作?靶點(diǎn):Microtubule/Tubulin作?通路:CellCycle/DNADamage;Cytoskeleton儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(28.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2859mL11.4294mL22.8587mL5mM0.4572mL2.2859mL4.5717mL10mM0.2286mL1.1429mL2.2859mL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:≥1.25mg/mL(2.86mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性S516(Compound22)CKD-516的活性代謝產(chǎn)物，?種有效的微管蛋?聚合抑制劑，其IC50值為4.29μM。S516具有顯著的抗腫瘤活性。IC50&TargetIC50:4.29μM(tubulinpolymerization)[1]體外研究S516haspotentcytotoxicitywithIC50sof4.8nM,42.8nMand24.9nMforHL-60,HCT116andHCT15cells,respectively[1].S516(Compound22;30nM;16hours;HL60cells)treatmemtcausessignificantarrestofcellsattheG2/Mphase,resultinginapoptosiswithconcomitantlossofG0/G1phase[1].CellCycleAnalysis[1]CellLine:HL60cellsConcentration:30nMIncubationTime:16hoursResult:CausedsignificantarrestofcellsattheG2/Mphase,resultinginapoptosiswithconcomitantlossofG0/G1phase.體內(nèi)研究S516(Compound22;5-10mg/kg;intraperitonealinjection;mice)treatmenthaspromisingantitumoractivity(inhibitionratio(IR)>63%)inhumanLX-1lungcancerandCX-1coloncancermousexenografts[1].AnimalModel:Micebearing3LLlungcancer[1]Dosage:5mg/kg,10mg/kgAdministration:IntraperitonealinjectionResult:Hadpromisingantitumoractivity(inhibitionratio(IR)>63%).REFERENCES[1].LeeJ,etal.IdentificationofCKD-516:apotenttubulinpolymerizationinhibitorwithmarkedantitumoractivityagainstmurineandhumansolidtumors.JMedChem.2010Sep9;53(17):6337-54.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu