Aderbasib-INCB007839-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAderbasibCat.No.:HY-10293CASNo.:791828-58-5Synonyms:INCB007839;INCB7839分?式:C??H??N?O?分?量:416.47作?靶點:MMP作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(240.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4011mL12.0057mL24.0113mL5mM0.4802mL2.4011mL4.8023mL10mM0.2401mL1.2006mL2.4011mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.00mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.00mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性Aderbasb(INCB007839)?種有效的、具有?服活性的、靶向特異性的低納爾ADAM10和ADAM17抑制劑。Aderbasb表現(xiàn)出強?的抗腫瘤活性，可?于癌癥研究，包括彌漫性?B細胞?霍奇?淋巴瘤，HER2+乳腺癌，膠質(zhì)瘤等。IC50&TargetADAM10ADAM17體外研究Aderbasibinhibitsthemetalloproteaseactivitythroughbindingtotheactivesiteofthemetalloproteinasedomain.Aderbasib(10-100μM)inhibitstheinteractionbetweenADAM17andsE2-Fc,astheconcentrationofthecompoundincreases,bindingofsE2-Fcdecreasedaccordingly,withalmostnobindingdetectedat100μMintrypsinizedPK15cells[2].Aderbasib(100-1000μM;pre-treatedfor0.5h)showsantiviraleffectagainstCSFVpseudovirusat100μMand1mMinPK15cells[2].體內(nèi)研究Aderbasib(intraperitonealinjection;50mg/kg;5daysperweekbeginningfourweeks;2weeks)blocksgliomagrowthofSU-pcGBM2NSGmicexenografts[1].INCB7839canbeformulatedin2%DMSO,2%Tween80,48%PEG300,48%waterasainjectionsolution.Thisisforliteraturereferenceonly[1].AnimalModel:NSGmice[1]Dosage:50mg/kgAdministration:Intraperitonealinjection;50mg/kg;5daysperweekbeginningfourweeks;2weeksResult:Robustlyinhibitedgrowthofpediatricglioblastomaorthotopicxenografts.REFERENCES[1].LoisWitters,etal.Synergisticinhibitionwithadualepidermalgrowthfactorreceptor/HER-2/neutyrosinekinaseinhibitorandadisintegrinandmetalloproteaseinhibitor.CancerRes.2008Sep1;68(17):7083-9.[2].FeiYuan,etal.ADAM17isanessentialattachmentfactorforclassicalswinefevervirus.PLoSPathog.2021Mar8;17(3):e1009393.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl