RHPS4-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERHPS4Cat.No.:HY-101089CASNo.:390362-78-4分⼦式:C₂₃H₂₀F₂N₂O₄S分⼦量:458.48作⽤靶点:Telomerase;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:1mg/mL(2.18mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1811mL10.9056mL21.8112mL5mM---------10mM---------请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.25mg/mL(2.73mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性RHPS4有效的端粒酶(telomerase)抑制剂(IC50=0.33μM)。RHPS4DNA损伤的诱导剂。IC50&TargetIC50:0.33μM(telomeraseintheTRAPassay)[1].体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedfor