Xevinapant-hydrochloride-AT-406-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXevinapanthydrochlorideCat.No.:HY-13208CASNo.:1071992-57-8Synonyms:AT-406hydrochloride;Debio1143hydrochloride;SM-406hydrochloride分⼦式:C₃₂H₄₄ClN₅O₄分⼦量:598.18作⽤靶点:IAP作⽤通路:Apoptosis储存⽅式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:175mg/mL(292.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6717mL8.3587mL16.7174mL5mM0.3343mL1.6717mL3.3435mL10mM0.1672mL0.8359mL1.6717mL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(sealedstorage,awayfrommoistureandlight)。-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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥8.75mg/mL(14.63mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥8.75mg/mL(14.63mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥8.75mg/mL(14.63mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Xevinapant(AT-406)hydrochloride⼀种有效的、⼝服⽣物可利⽤的Smac模拟物，也细胞凋亡蛋⽩(IAPs)抑制剂的拮抗剂。Xevinapanthydrochloride与XIAP、cIAP1和cIAP2蛋⽩结合，Ki分别为66.4、1.9和5.1nM。Xevinapanthydrochloride在⽆细胞功能测定中有效拮抗XIAPBIR3蛋⽩，诱导细胞cIAP1蛋⽩的快速降解，并抑制各种⼈类癌细胞系中的癌细胞⽣长。Xevinapanthydrochloride在诱导异种移植肿瘤细胞凋亡⽅⾮常有效。IC50&TargetcIAP1cIAP2XIAP1.9nM(Ki)5.1nM(Ki)66.4nM(Ki)体外研究Xevinapant(AT-406)hydrochloridepotentlyinhibitscellgrowthintheMDA-MB-231breastandSK-OV-3ovariancancercelllineswithIC50=144nMand142nM,respectively.Xevinapant(0-3μM;0-48horus)hydrochlorideeffectivelyinducescelldeathinatime-anddose-dependentmanner[1].体内研究Xevinapant(AT-406)hydrochlorideisveryeffectiveininhibitionoftumorgrowthintheMDA-MB-231xenograftmodel,andhasminimaltoxicitytoanimals[1].Xevinapanthydrochlorideevaluatedforitspharmacokinetic(PK)propertiesinmice,rats,non-humanprimatesanddogs[1].AnimalModel:SCIDmicebearingMDA-MB-231xenografttumors[1]Dosage:30and100mg/kgAdministration:p.o.;5daysaweekfor2weeksResult:Stronglyinhibitstumorgrowthat30and100mg/kgandcompletelyinhibitstumorgrowthduringthetreatmentwith100mg/kg.户使⽤本产品发表的科研⽂献•JMedChem.2019Oct24;62(20):9188-9200.•BiochimBiophysActaMolBasisDis.2019Jun26;1865(10):2618-2632.•Viruses.2021,13(12),2490.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].CaiQ,SunH,PengY,etal.Apotentandorallyactiveantagonist(SM-406/AT-406)ofmultipleinhibitorofapoptosisproteins(IAPs)inclinicaldevelopmentforcancertreatment.JMedChem.2011;54(8):2714-2726.[2].BrunckhorstMK,etal.AT-406,anorallyactiveantagonistofmultipleinhibitorofapoptosisproteins,inhibitsprogressionofhumanovariancancer.CancerBiolTher.2012;13(9):804-811.McePdfHeightCaution:Producthasnotbeenfully