RHPS4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERHPS4Cat.No.:HY-101089CASNo.:390362-78-4分?式:C??H??F?N?O?S分?量:458.48作?靶點:Telomerase;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:1mg/mL(2.18mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1811mL10.9056mL21.8112mL5mM---------10mM---------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:1.25mg/mL(2.73mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性RHPS4有效的端粒酶(telomerase)抑制劑(IC50=0.33μM)。RHPS4DNA損傷的誘導(dǎo)劑。IC50&TargetIC50:0.33μM(telomeraseintheTRAPassay)[1].體外研究RHPS4couldsensitizetumorcellstoanticanceragentsthatactviadisparatemechanisms[1].RHPS4(0.5-1μM,15days)inducesasenescent-likegrowtharrestinMCF-7cells[1].RHPS4(1μM,4days)inducesphosphorylationofH2AXintransformedandtumorcells[2].CellProliferationAssay[1]CellLine:MCF-7,MCF-7vectorcontrol,andMCF-7c81cells.Concentration:0,0.2,0.5,or1μM.IncubationTime:7days.Result:Inhibitedcellproliferation.體內(nèi)研究RHPS4(15mg/kg,iv,15days)treatmentproducesamarkedinhibitionoftumorweight(tumorweightinhibition[TWI]about80%;P<0.001)inaveryshorttime,andthiseffectpersistsforatleast30days.Acompletetumorresponseisobservedin80%ofmice,and40%arecured[2].Inalltheothertumorxenografts,RHPS4treatmentproducesabout50%(P<0.001)TWIatthenadiroftheeffectand,moreimportant,resultsinadelayoftumorgrowthofabout15(M14andPC3)and10(HT29andH460)days[2].AnimalModel:CD-1malenude(nu/nu)mice,6–8weeksoldandweighing22-24g(H460,CG5andHT29,PC3andM14cancermodels)[2].Dosage:15mg/kg.Administration:IV,dailyfor15consecutivedays.Result:Activeasasingleagentonallthetumorsanalyzed.CG5breastxenograftsresultedinthemostsensitivetumor.REFERENCES[1].JenniferCCookson,etal.PharmacodynamicsoftheG-quadruplex-stabilizingtelomeraseinhibitor3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridiniummethosulfate(RHPS4)invitro:activityinhumantumorcellscorrelateswithtelomerelengthandcanbeenhanced,orantagonized,withcytotoxicagents.MolPharmacol.2005Dec;68(6):1551-8.[2].EricaSalvati,etal.TelomeredamageinducedbytheG-quadruplexligandRHPS4hasanantitumoreffect.JClinInvest.2007Nov;117(11):3236-47.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedfor