AZD3229-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZD3229Cat.No.:HY-112802CASNo.:2248003-60-1分⼦式:C₂₄H₂₆FN₇O₃分⼦量:479.51作⽤靶点:c-Kit作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:40mg/mL(83.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0855mL10.4273mL20.8546mL5mM0.4171mL2.0855mL4.1709mL10mM0.2085mL1.0427mL2.0855mL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%salineSolubility:4mg/mL(8.34mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:4mg/mL(8.34mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:4mg/mL(8.34mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性AZD3229⼀种有效的、⼴泛的突变型酪氨酸激酶受体(KIT)抑制剂，可⽤于开发研究胃肠道间质瘤。IC50&TargetKIT[1].体外研究AZD3229isapotent,pan-KITmutantinhibitorwithpotentsingledigitnMgrowthinhibitionagainstadiversepanelofmutantKITdrivenBa/F3celllines(GI50=1-50nM).AZD3229demonstratespotentsingledigitnMgrowthinhibitionacrossabroadcellpanel,withgoodmargintoKDR-driveneffects.SelectivityoverKDRcanberationalisedpredominantlybytheinteractionofwatermoleculeswiththeproteinandligandintheactivesiteanditskinomeselectivityissimilartothebestoftheapprovedGISTagents[1].REFERENCES[1].KettleJG,etal.DiscoveryofN-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide(AZD3229),aPotentPan-KITMutantInhibitorfortheTreatmentofGastrointestinalStromalTumors.JMedMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T