Xevinapant-hydrochloride-AT-406-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEXevinapanthydrochlorideCat.No.:HY-13208CASNo.:1071992-57-8Synonyms:AT-406hydrochloride;Debio1143hydrochloride;SM-406hydrochloride分?式:C??H??ClN?O?分?量:598.18作?靶點(diǎn):IAP作?通路:Apoptosis儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:175mg/mL(292.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6717mL8.3587mL16.7174mL5mM0.3343mL1.6717mL3.3435mL10mM0.1672mL0.8359mL1.6717mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)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:≥8.75mg/mL(14.63mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥8.75mg/mL(14.63mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥8.75mg/mL(14.63mM);ClearsolutionBIOLOGICALACTIVITY?物活性Xevinapant(AT-406)hydrochloride?種有效的、?服?物可利?的Smac模擬物，也細(xì)胞凋亡蛋?(IAPs)抑制劑的拮抗劑。Xevinapanthydrochloride與XIAP、cIAP1和cIAP2蛋?結(jié)合，Ki分別為66.4、1.9和5.1nM。Xevinapanthydrochloride在?細(xì)胞功能測(cè)定中有效拮抗XIAPBIR3蛋?，誘導(dǎo)細(xì)胞cIAP1蛋?的快速降解，并抑制各種?類癌細(xì)胞系中的癌細(xì)胞?長(zhǎng)。Xevinapanthydrochloride在誘導(dǎo)異種移植腫瘤細(xì)胞凋亡??常有效。IC50&TargetcIAP1cIAP2XIAP1.9nM(Ki)5.1nM(Ki)66.4nM(Ki)體外研究Xevinapant(AT-406)hydrochloridepotentlyinhibitscellgrowthintheMDA-MB-231breastandSK-OV-3ovariancancercelllineswithIC50=144nMand142nM,respectively.Xevinapant(0-3μM;0-48horus)hydrochlorideeffectivelyinducescelldeathinatime-anddose-dependentmanner[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JMedChem.2019Oct24;62(20):9188-9200.?BiochimBiophysActaMolBasisDis.2019Jun26;1865(10):2618-2632.?Viruses.2021,13(12),2490.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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