S55746-BCL201-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemES55746Cat.No.:HY-117288CASNo.:1448584-12-0Synonyms:BCL201分?式:C??H??N?O?分?量:710.82作?靶點:Bcl-2Family作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(70.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.4068mL7.0341mL14.0683mL5mM0.2814mL1.4068mL2.8137mL10mM0.1407mL0.7034mL1.4068mL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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(3.52mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5.75mg/mL(8.09mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.52mM);ClearsolutionBIOLOGICALACTIVITY?物活性S55746(BCL201)?種有效、可?服、選擇性的BCL-2抑制劑，其Ki值和Kd值分別為1.3nM和3.9nM。S55746(BCL201)具有抗腫瘤活性且毒性低。IC50&TargetBcl-2Bcl-xLBcl-2Bcl-xL1.3nM(Ki)520nM(Ki)3.9nM(Kd)186nM(Kd)體外研究S55746(0-1μM)potentlyandselectivelyinducescelldeath[1].S55746selectivelyinducesapoptosisthroughBCL-2inhibitioninaBAX/BAK-dependentmanner[1].WesternBlotAnalysis[1]CellLine:H146andRS4;11celllines.Concentration:0,0.1,0.3and1μM.IncubationTime:72hours.Result:PotentlyinducedRS4;11cellkillingafter72hoftreatmentwithanIC50of71.6nM.體內(nèi)研究S55746isahighlyefficaciousandwell-tolerated(evenatdosesupto300mg/kg)orallyactiveBCL-2inhibitor[1].S55746(20-100mg/kg,p.o.)inhibitsxenograftgrowthinRS4;11andToledomodelstime-anddose-dependently[1].AnimalModel:FemaleSCID/beigemiceimplantedsubcutaneouslywith3×106ToledoorRS4;11[1].Dosage:20,50,100mg/kg.Administration:Oralgavagedailyfor7consecutivedays.Result:Inducedsignificantanti-tumoractivitytime-anddose-dependently.AnimalModel:SCID/beigefemalemicewithRS4;11tumorxenografts[1].Dosage:25and100mg/kg.Administration:Singleoralgavagetreatment.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Didnotinduceplateletlossinvivoat25and100mg/kg.戶使?本產(chǎn)品發(fā)表的科研?獻?BiomedPharmacother.2021Jan1;135:111213.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CasaraP,etal.S55746isanovelorallyactiveBCL-2selectiveandpotentinhibitorthatimpairshematologicaltumorgrowth.Oncotarget.2018Apr13;9(28):20075-20088.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical