Aderbasib-INCB007839-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAderbasibCat.No.:HY-10293CASNo.:791828-58-5Synonyms:INCB007839;INCB7839分⼦式:C₂₁H₂₈N₄O₅分⼦量:416.47作⽤靶点:MMP作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(240.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4011mL12.0057mL24.0113mL5mM0.4802mL2.4011mL4.8023mL10mM0.2401mL1.2006mL2.4011mL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>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.00mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.00mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.00mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Aderbasb(INCB007839)⼀种有效的、具有⼝服活性的、靶向特异性的低纳尔ADAM10和ADAM17抑制剂。Aderbasb表现出强⼤的抗肿瘤活性，可⽤于癌症研究，包括弥漫性⼤B细胞⾮霍奇⾦淋巴瘤，HER2+乳腺癌，胶质瘤等。IC50&TargetADAM10ADAM17体外研究Aderbasibinhibitsthemetalloproteaseactivitythroughbindingtotheactivesiteofthemetalloproteinasedomain.Aderbasib(10-100μM)inhibitstheinteractionbetweenADAM17andsE2-Fc,astheconcentrationofthecompoundincreases,bindingofsE2-Fcdecreasedaccordingly,withalmostnobindingdetectedat100μMintrypsinizedPK15cells[2].Aderbasib(100-1000μM;pre-treatedfor0.5h)showsantiviraleffectagainstCSFVpseudovirusat100μMand1mMinPK15cells[2].体内研究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