AG1024-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEAG1024Cat.No.:HY-10253CASNo.:65678-07-1分?式:C??H??BrN?O分?量:305.17作?靶點(diǎn):IGF-1R;InsulinReceptor;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥50mg/mL(163.84mM)掃描?維碼，*"≥"meanssoluble,butsaturationunknown.運(yùn)?溶解?案計算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2769mL16.3843mL32.7686mL5mM0.6554mL3.2769mL6.5537mL10mM0.3277mL1.6384mL3.2769mL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，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(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.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(8.19mM);Clearsolution此?案可獲得≥2.5mg/mL(8.19mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemEBIOLOGICALACTIVITY?物活性AG1024(TyrphostinAG1024)?種可逆的，競爭性和選擇性的胰島素樣?長因?-1受體(IGF-1R)抑制劑，IC50為7μM。AG1024抑制胰島素受體(IR)的磷酸化(IC50=57μM)。AG1024誘導(dǎo)細(xì)胞凋亡(apoptosis)并具有抗癌活性。IC50&TargetIC50:7μM(IGF1R)and57μM(IR)[1][2]體外研究AG1024(TyrphostinAG1024;2-10μM;1-5days)showsadose-dependentinhibitionofcellproliferation[1].AG1024(1-5μM;1-3days)inducesUT7-9andBaf3-p210cellsapoptosis[1].AG1024(2μM;6,12hours)downregulatesphospho-Akt,Bcr-AblandupregulatesDNA-PKcs[1].CellProliferationAssay[1]CellLine:UT7-9andBaf3-p210cellsConcentration:2,5,10μMIncubationTime:1,3,5daysResult:Showedadose-dependentinhibitionofcellproliferation.ApoptosisAnalysis[1]CellLine:UT7-9andBaf3-p210cellsConcentration:1,3,5μMIncubationTime:1,2,3daysResult:Inducedapoptosis.WesternBlotAnalysis[1]CellLine:UT7-9andBa/F3-p210cellsConcentration:2μMIncubationTime:6,12hoursResult:Downregulatedphospho-Akt,Bcr-AblandupregulatedDNA-PKcs.體內(nèi)研究AG1024(TyrphostinAG1024;30μg;i.p.;perday;for2weeks)significantlydelaysthetumourgrowth[1].AnimalModel:Femalenudemice(6-8weeksold)[1]Dosage:30μg2/3www.MedChemEwww.MedChemEAdministration:IP;perday;for2weeksResult:Significantlydelayedthetumourgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?BiomedPharmacother.2017Nov;95:1346-1358.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PárrizasM,etal.SpecificinhibitionofIGF-1RandIRtyrosinekinaseactivityandbiologicalfunctionbytyrphostins.Endocrinology.1997Apr;138(4):1427-33.[2].DeutschE,etal.TyrosinekinaseinhibitorAG1024exertsantileukaemiceffectsonSTI571-resistantBcr-AblexpressingcellsanddecreasesAKTphosphorylation.BrJCancer.2004Nov1;91(9):1735-41.McePdfHeight關(guān)注MCE中國公眾號，

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